Al-Azhar University

Since the outbreak of the COVID-19 (coronavirus disease 19) pandemic, researchers have been trying to investigate several active compounds found in plants that have the potential to inhibit the proliferation of SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2). The present study aimed to evaluate bioactive compounds found in plants using a molecular docking approach to inhibit the main protease (Mpro) and spike (S) glycoprotein of SARS-CoV-2. The evaluation was performed on the docking scores calculated using AutoDock Vina (AV) as a docking engine. A rule of five (Ro5) was calculated to determine whether a compound meets the criteria as an active drug orally in humans. The determination of the docking score was performed by selecting the best conformation of the protein-ligand complex that had the highest affinity (most negative Gibbs’ free energy of binding/ <a:math xmlns:a="http://www.w3.org/1998/Math/MathML" id="M1"> <a:mi mathvariant="normal">Δ</a:mi> <a:mi>G</a:mi> </a:math> ). As a comparison, nelfinavir (an antiretroviral drug), chloroquine, and hydroxychloroquine sulfate (antimalarial drugs recommended by the FDA as emergency drugs) were used. The results showed that hesperidin, nabiximols, pectolinarin, epigallocatechin gallate, and rhoifolin had better poses than nelfinavir, chloroquine, and hydroxychloroquine sulfate as spike glycoprotein inhibitors. Hesperidin, rhoifolin, pectolinarin, and nabiximols had about the same pose as nelfinavir but were better than chloroquine and hydroxychloroquine sulfate as Mpro inhibitors. This finding implied that several natural compounds of plants evaluated in this study showed better binding free energy compared to nelfinavir, chloroquine, and hydroxychloroquine sulfate, which so far are recommended in the treatment of COVID-19. From quantum chemical DFT calculations, the ascending order of chemical reactivity of selected compounds was pectolinarin &gt; hesperidin &gt; rhoifolin &gt; morin &gt; epigallocatechin gallate. All isolated compounds’ C=O regions are preferable for an electrophilic attack, and O-H regions are suitable for a nucleophilic attack. Furthermore, Homo-Lumo and global descriptor values indicated a satisfactory remarkable profile for the selected compounds. As judged by the RO5 and previous study by others, the compounds kaempferol, herbacetin, eugenol, and 6-shogaol have good oral bioavailability, so they are also seen as promising candidates for the development of drugs to treat infections caused by SARS-CoV-2. The present study identified plant-based compounds that can be further investigated in vitro and in vivo as lead compounds against SARS-CoV-2.

BACKGROUND: The introduction of a stapling technique for the treatment of haemorrhoids has the potential for less postoperative pain, a short operating time and an early return to full activity. The outcome of stapled haemorrhoidectomy was compared with that of current standard surgery in a randomized controlled study. METHODS: Two hundred patients were randomized to either stapled haemorrhoidectomy (n = 100) or Milligan-Morgan haemorrhoidectomy (n = 100) between March 1997 and December 1998. Each patient received standardized postoperative analgesic and laxative regimens, and completed a linear analogue pain score every 6 h during the first day after operation, after the first motion and daily until the end of the first week. Operating time, frequency of postoperative analgesic intake, hospital stay, time to return to normal activity and postoperative complications were also recorded. RESULTS: The mean(s.d.) age of patients in the stapled and surgical groups was 44.1(3.2) and 49.1(12.2) years respectively. The stapled group had a shorter operating time, less frequent postoperative analgesia intake, shorter hospital stay and earlier return to normal activity. Early and late complications, and functional outcome were better in the stapled group. CONCLUSION: Use of a circular stapler in the treatment of haemorrhoidal disease was safe, and was associated with fewer complications than conventional haemorrhoidectomy.

Abstract Purpose This in vitro study evaluated the flexural strength, impact strength, hardness, and surface roughness of 3D‐printed denture base resin subjected to thermal cycling treatment. Materials and Methods According to ISO 20795‐1:2013 standards, 120 acrylic resin specimens (40/flexural strength test, 40/impact strength, and 40/surface roughness and hardness test, n = 10) were fabricated and distributed into two groups: heat‐polymerized; (Major.Base.20) as control and 3D‐printed (NextDent) as experimental group. Half of the specimens of each group were subjected to 10,000 thermal cycles of 5 to 55°C simulating 1 year of clinical use. Flexural strength (MPa), impact strength (KJ/m 2 ), hardness (VHN), and surface roughness (μm) were measured using universal testing machine, Charpy's impact tester, Vickers hardness tester, and profilometer, respectively. Data were analyzed by ANOVA and Tukey honestly significant difference (HSD) test (α = 0.05). Results The values of flexural strength (MPa) were 86.63 ± 1.0 and 69.15 ± 0.88; impact strength (KJ/m 2 )—6.32 ± 0.50 and 2.44 ± 0.31; hardness (VHN)—41.63 ± 2.03 and 34.62 ± 2.1; and surface roughness (μm)—0.18 ± 0.01 and 0.12 ± 0.02 for heat‐polymerized and 3D‐printed denture base materials, respectively. Significant differences in all tested properties were recorded between heat‐polymerized and 3D‐printed denture base materials ( P &lt; 0.001). Thermal cycling significantly lowered the flexural strength (63.93 ± 1.54 MPa), impact strength (2.40 ± 0.35 KJ/m 2 ), and hardness (30.17 ± 1.38 VHN) of 3D‐printed resin in comparison to thermal cycled heat‐polymerized resin, but surface roughness showed non‐significant difference ( p = 0.262). Conclusion 3D‐printed resin had inferior flexural strength, impact strength, and hardness values than heat‐polymerized resin, but showed superior surface roughness. Temperature changes (thermal cycling) significantly reduced the hardness and flexural strength and increased surface roughness, but did not affect the impact strength.

OBJECTIVE: To evaluate in vitro and in vivo effects of Moses technology in Holmium laser and to compare it with the Regular mode in terms of lithotripsy efficiency and laser-tissue interactions. METHODS: Pulse™ P120H holmium laser system together with Moses D/F/L fibers were used to compare the Regular mode with the Moses modes in stone retropulsion by using a high-speed camera, and stone ablation efficiency. In addition, a porcine ureteroscopy model was used to assess stone fragmentation and dusting as well as laser-tissue interaction with the ureteral wall. RESULTS: After a laser pulse, in vitro stone displacement experiments showed a significant reduction in retropulsion when using the Moses mode. The stone movement was reduced by 50 times at 0.8 J and 10 Hz (p < 0.01). The pronounced reduction of retropulsion in the Moses mode was clearly observed during fragmentation setting (high energy) and dusting (low energy, high Hz). In addition, stone fragmentation tests showed that the Moses modes resulted in a significantly higher ablation volume when compared with the Regular mode (160% higher; p < 0.001). In vivo assessment also supported the reduction in retropulsion when treating stones in the porcine kidney. Histological analysis of the porcine ureter after direct lasing in the Moses mode suggested less damage than in the Regular mode. CONCLUSIONS: The Moses technology resulted in more efficient laser lithotripsy, in addition to significantly reduced stone retropulsion, and displayed a margin of safety that may result in a shorter procedural time and safer lithotripsy.

Gentamicin (GM) is an antibiotic widely used in treating severe gram-negative infections. However, its clinical use is limited by its nephrotoxicity. Several lines of evidence indicate that free radicals are important mediators of gentamicin nephrotoxicity. Therefore, the aim of this work was to investigate the possible protective effect of the flavonoid quercetin, an antioxidant, on gentamicin-induced nephrotoxicity. For this purpose, rats were divided into four groups. First group served as a control and injected with the normal saline, second group was injected with quercetin (50 mg/kg/d, per os) for 7 d, third group was injected with gentamicin (80 mg/kg/d, intraperitoneally) for 7 d and the fourth group of animals was injected with quercetin plus gentamicin simultaneously for 7 d. Total protein levels were estimated in 24-h urine samples to assess kidney dysfunction. The rats were sacrificed on the seventh day and kidneys were collected for histopathological studies. Blood urea nitrogen (BUN) and creatinine levels were measured in the blood. Moreover, glutathione (GSH), lipid peroxide (TBARS) levels, superoxide dismutase (SOD) and catalase (CAT) activities were determined in renal tissues. GM-treated rats showed early kidney dysfunction as urinary total protein, BUN and serum creatinine levels were significantly increased. The significant decrease in GSH levels, SOD, CAT activities and increase in TBARS levels, indicated that GM-induced nephrotoxicity was mediated through oxidative stress reactions. Histopathological examination of GM-treated rats revealed degenerative changes in glomeruli and tubules. On the other hand, simultaneous administration of quercetin plus gentamicin protected kidney tissues against nephrotoxic effects of gentamicin as evidenced from amelioration of histopathological changes and normalization of kidney biochemical parameters.

Abstract Background: In mice, bacteria from the mouth can translocate to the pancreas and impact pancreatic cancer progression. In humans, oral bacteria associated with periodontal disease have been linked to pancreatic cancer risk. It is not known if DNA bacterial profiles in the pancreas and duodenum are similar within individuals. Methods: Tissue samples were obtained from 50 subjects with pancreatic cancer or other conditions requiring foregut surgery at the Rhode Island Hospital (RIH), and from 34 organs obtained from the National Disease Research Interchange. 16S rRNA gene sequencing was performed on 189 tissue samples (pancreatic duct, duodenum, pancreas), 57 swabs (bile duct, jejunum, stomach), and 12 stool samples. Results: Pancreatic tissue samples from both sources (RIH and National Disease Research Interchange) had diverse bacterial DNA, including taxa typically identified in the oral cavity. Bacterial DNA across different sites in the pancreas and duodenum were highly subject specific in both cancer and noncancer subjects. Presence of genus Lactobacillus was significantly higher in noncancer subjects compared with cancer subjects and the relative abundance of Fusobacterium spp., previously associated with colorectal cancer, was higher in cancer subjects compared with noncancer subjects. Conclusions: Bacterial DNA profiles in the pancreas were similar to those in the duodenum tissue of the same subjects, regardless of disease state, suggesting that bacteria may be migrating from the gut into the pancreas. Whether bacteria play a causal role in human pancreatic cancer needs to be further examined. Impact: Identifying bacterial taxa that differ in cancer patients can provide new leads on etiologically relevant bacteria.

The present work aims to prepare an ecofriendly and effective material for adsorption of heavy metals, especially iron and manganese from polluted water. Chitosan nanoparticles were prepared from the extracted chitosan of shrimp shells waste using a traditional ionic gelation method in presence of sodium tripolyphosphate as a cross-linker. To confirm the polymer structure and its characteristics, the prepared nanoparticles were characterized using FT-IR, X-Ray diffraction, TEM and SEM. Molecular weight, the degree of de-acetylation, ash content, particle size and zeta potential values were 3923 D, 75 %, 4 %, 331 nm and +38 mv, respectively. A batch equilibrium experiments were carried out to evaluate the chitosan nanoparticles as adsorbents of Fe (II) and Mn (II) ions from aqueous solutions. The removal efficiency and adsorption capacity were studied at different contact times, pH of the sorption medium, and initial metal ion concentration in the feed solution. The removal efficiency and maximum adsorption capacity of Fe (II) and Mn (II) were 99.8, 116.2 mg/g and 95.3%, 74.1mg/g, respectively. From the adsorption isotherm and kinetic studies, it was found that the Langmuir and the pseud-second order models, respectively, were more fitted in this study.

AIM: One of the defining features of the liver is the capacity to maintain a constant size despite injury. Extrahepatic stem cells especially bone marrow-derived stem cells are thought to undertake an important role in liver repopulation. This study was carried out to evaluate the outcome of autologous bone marrow-derived hepatocytes transplantation in patients with end-stage liver cell failure due to chronic hepatitis C. METHODS: Forty patients were included, divided into two groups. Group I: 20 patients receiving autologous bone marrow-derived mesenchymal stem cells stimulated to hepatic lineage. They were subdivided into two groups regarding the route of transplantation: intrasplenic (10) and intrahepatic (10). Group II: included 20 patients who received traditional supportive treatment. Patients were followed up using examination, laboratory investigations, abdominal ultrasonography, and evaluated by Child score, Model for End Stage Liver Disease score, fatigue scale, and performance status. RESULTS: The results showed significant improvement in group I regarding ascites, lower limb edema, and serum albumin, over the control group. Group I also showed statistically significant improvement in Child score, Model for End Stage Liver Disease score, fatigue scale, and performance status over the controls. No difference was observed between intrahepatic and intrasplenic groups. CONCLUSION: This study demonstrated the safety and short-term efficacy of autologous bone marrow-derived mesenchymal stem cell injection in liver cell failure. Further study is necessary to standardize the cell dose, determine the life span of the injected cells, and detect the appearance of long-term complications.

BACKGROUND: The tricuspid valve (TV) is a complex structure. Unlike the aortic and mitral valve it is not possible to visualize all TV leaflets simultaneously in one cross-sectional view by standard two-dimensional echocardiography (2DE) either transthoracic or transesophageal due to the position of TV in the far field. AIM: Quantitative and qualitative assessment of the normal TV using real-time 3-dimensional echocardiography (RT3DE). METHODS: RT3DE was performed for 100 normal adults (mean age 30 +/- 9 years, 65% males). RT3DE visualization was evaluated by 4-point score (1: not visualized, 2: inadequate, 3: sufficient, and 4: excellent). Measurements included TV annulus diameters (TAD), TV area (TVA), and commissural width. RESULTS: In 90% of patients with good 2DE image quality, it was possible to analyse TV anatomy by RT3DE. A detailed anatomical structure including unique description and measurement of tricuspid annulus shape and size, TV leaflets shape, and mobility, and TV commissural width were obtained in majority of patients. Identification of each TV leaflet as seen in the routine 2DE views was obtained. CONCLUSION: RT3DE of the TV is feasible in a large number of patients. RT3DE may add to functional 2DE data in description of TV anatomy and providing highly reproducible and actual reality (anatomical and functional) measurements.

The present investigation was carried out to study the cytological effects of the herbicide atrazine on Allium cepa and Vicia faba with respect to the cell cycle response, mitotic index, chromosome aberrations and nucleic acids content. The root of young seedlings of V. faba and adventitious roots of A. cepa were treated with the following concentrations : 25%, 50%, 75% and 100% of the recommended dose (3.75 g/l) for 4, 8, 12, 24 h. The results indicated that atrazine herbicide reduced the mitotic division in both plants compared to the respective control. Mitotic index values were progressively decreased with increased the concentration and treatment time. In V. faba, the treatment with the concentration of 100% for each treatment time (4, 8, 12, 24 h) was toxic, but in A. cepa, the same concentration with 24 h was only toxic. The percentage of the reduction in MI values in V. faba was higher than that in A. cepa. Also, it has been clearly observed that the inhibition of mitotic division was associated with reduction in DNA and RNA contents in both treated plants root tips. This may point out that the inhibition of mitotic activity is due to a deficiency of DNA in the nucleus. The increased percentage of prophase in both plants was accompanied by decreased percentages of the other mitotic phase. The total percentage of aberrations increased with the increasing the concentration of atrazine herbicide and the period of treatment. The total percentage of aberrations in A. cepa was higher than that in V. faba for each treatment. Different abnormal mitotic figures were observed in all mitotic phases. Such types of abnormalities were stickiness, lagging, C-mitosis, bridges, irregular prophase, unequal distribution, fragments and a few cells with micronucleus at interphase stage.

Background: Polymethyl methacrylate (PMMA) is widely used for the fabrication of removable prostheses. Recently, zirconium oxide nanoparticles (nano-ZrO 2 ) have been added to improve some properties of PMMA, but their effect on the optical properties and tensile strength are neglected. Objective: The aim of this study was to investigate the effect of nano-ZrO 2 addition on the translucency and tensile strength of the PMMA denture base material. Materials and methods: Eighty specimens (40 dumbbell-shaped and 40 discs) were prepared out of heat-polymerized acrylic resin and divided into four groups per test (n=10). The control group for each test included unreinforced acrylic, while the test groups were reinforced with 2.5, 5, and 7.5 wt% nano-ZrO 2 . Acrylic resin was mixed according to manufacturer’s instructions, packed, and processed by conventional method. After polymerization, all specimens were finished, polished, and stored in distilled water at 37°C for 48±2 hours. Tensile strength (MPa) was evaluated using the universal testing machine while the specimens’ translucency was examined using a spectrophotometer. Statistical analysis was carried out by SPSS using the paired sample t -test ( p ≤0.05). A scanning electron microscope was used to analyze the morphological changes and topography of the fractured surfaces. Results: This study showed that the mean tensile strength of the PMMA in the test groups of 2.5%NZ, 5%NZ, and 7.5%NZ was significantly higher than the control group. The tensile strength increased significantly after nano-ZrO 2 addition, and the maximum increase seen was in the 7.5%NZ group. The translucency values of the experimental groups were significantly lower than those of the control group. Within the reinforced groups, the 2.5%NZ group had significantly higher translucency values when compared to the 5%NZ and 7.5%NZ groups. Conclusion: The addition of nano-ZrO 2 increased the tensile strength of the denture base acrylic. The increase was directly proportional to the nano-ZrO 2 concentration. The translucency of the PMMA was reduced as the nano-ZrO 2 increased. Clinical significance: Based on the results of the current study, the tensile strength was improved with different percentages of nano-ZrO 2 additions. However, translucency was adversely affected. Therefore, it is important to determine the appropriate amount of reinforcing nano-ZrO 2 that will create a balance between achieved properties – mechanical and optical. Keywords: denture base, PMMA, tensile strength, translucency, zirconium oxide nanoparticles

Background: Repeated fracture of the denture base is a common problem in prosthodontics, and it represents a nuisance and a time sink for the clinician. Therefore, the possibility of increasing repair strength using new reinforcement materials is of great interest to prosthodontists. Aim of the study: This study aimed to evaluate the effects of incorporation of zirconia nanoparticles (nano-ZrO 2 ) on the flexural strength and impact strength of repaired polymethyl methacrylate (PMMA) denture bases. Materials and methods: One hundred eighty specimens of heat-polymerized acrylic resin were fabricated (90 for each test) and divided into three main groups: one control group (intact specimens) and two groups divided according to surface design (45° bevels and butt joints), in which specimens were prepared in pairs to create 2.5 mm gaps. Nano-ZrO 2 was added to repair resin in 2.5 wt%, 5 wt%, and 7.5 wt% concentrations of acrylic powder. A three-point bending test was used to measure flexural strength, and a Charpy-type test was used to measure impact strength. Scanning electron microscopy was used to analyze the fracture surfaces and nano-ZrO 2 distribution. The results were analyzed with a paired sample t -test and an unpaired t -test, with a P-value of ≤0.05 being significant. Results: Incorporation of nano-ZrO 2 into the repair resin significantly increased flexural strength ( P <0.05). The highest value was found in the bevel group reinforced with 7.5% nano-ZrO 2 , whereas the lowest value was found in the butt group reinforced with 2.5% nano-ZrO 2 . The impact strength values of all repaired groups were significantly lower than those of the control group ( P <0.05). Among repaired groups, the higher impact strength value was seen in the butt group reinforced with 2.5% nano-ZrO 2 . The bevel joint demonstrated mainly cohesive failure, whereas the butt joint demonstrated mainly adhesive failure. Conclusion: Incorporation of nano-ZrO 2 into the repair resin improved the flexural strength of repaired denture bases, whereas it decreased impact strength, especially with high nano-ZrO 2 concentrations. Keywords: denture repair, flexural strength, impact strength, PMMA, ZrO 2 nanoparticles

New Trends in Architectural Education presents a wide range of innovative concepts and practical methods for teaching architectural design, together with examples of different studio teaching. It traces the roots of architectural education, several disparate ideas, and strategies of design teaching practices including the Ecole Des Beaux-Arts and the Bauhaus. This book offers a comparative analysis of contemporary trends that are committed to shaping and identifying studio objectives and processes. It explores different aspects of studio teaching and what impact they have on attitudes, skills, methods, and tools of designers. New Trends in Architectural Education calls for a fresh look at design education in architecture, where the author proposes an approach within which architectural educators can envision and evaluate the needs of future architects and the type of education that satisfies those needs.

In plants, root nitrate uptake systems are under systemic feedback repression by the N satiety of the whole organism, thus adjusting the N acquisition capacity to the N demand for growth; however, the underlying molecular mechanisms are largely unknown. We previously isolated the Arabidopsis high nitrogen-insensitive 9-1 (hni9-1) mutant, impaired in the systemic feedback repression of the root nitrate transporter NRT2.1 by high N supply. Here, we show that HNI9 encodes Arabidopsis INTERACT WITH SPT6 (AtIWS1), an evolutionary conserved component of the RNA polymerase II complex. HNI9/AtIWS1 acts in roots to repress NRT2.1 transcription in response to high N supply. At a genomic level, HNI9/AtIWS1 is shown to play a broader role in N signaling by regulating several hundred N-responsive genes in roots. Repression of NRT2.1 transcription by high N supply is associated with an HNI9/AtIWS1-dependent increase in histone H3 lysine 27 trimethylation at the NRT2.1 locus. Our findings highlight the hypothesis that posttranslational chromatin modifications control nutrient acquisition in plants.

Medical image segmentation is important for disease diagnosis and support medical decision systems. The study proposes an efficient 3D semantic segmentation deep learning model “3D-DenseUNet-569” for liver and tumor segmentation. The proposed 3D-DenseUNet-569 is a fully 3D semantic segmentation model with a significantly deeper network and lower trainable parameters. The proposed model adopts Depthwise Separable Convolution (DS-Conv) as opposed to traditional convolution. The DS-Conv significantly decreases GPU memory requirements and computational cost and achieves high performance. The proposed 3D-DenseUNet-569 utilizes DensNet connections and UNet links, which preserve low-level features and produce effective results. The results of experimental study on the standard LiTS dataset demonstrate that the 3D-DenseNet-569 model is effective and efficient with respect to related studies.

Lactic acidosis is a serious, metabolic complication that may occur due to metformin hydrochloride (MH) accumulation during the treatment of diabetes mellitus. The aim of this study is to enhance the bioavailability of MH by oral route. Span 40 and cholesterol were used for the preparation of MH-loaded niosomes by the reverse phase evaporation technique. Dicetyl phosphate (DCP) and 1,2-dioleoyl-3-trimethylammonium-propane chloride salt (DOTAP) were used to obtain negatively and positively charged vesicles, respectively. The mean particle size ranged from 223.5 to 384.6 nm and the MH-loaded niosomes' surface was negatively charged in the absence of charge inducing agents (-16.6 ± 1.4 mV) and also with DCP (-26.9 ± 1.0 mV), while it was positively charged (+8.7 ± 1.2 mV) with DOTAP. High entrapment efficiency was observed in all the formulations. MH-loaded niosomes were found to effectively sustain the release of drug, particularly with positively charged niosomes. The bioavailability of MH-loaded niosomes was assessed by measuring the serum values of glucose and metformin in the different studied Wistar rats groups. The pharmacokinetic data of MH-loaded niosomal preparation showed a significant prolongation and increased intensity of hypoglycemic effect more than that observed for free MH solution. Area above the blood glucose levels-time curve (AAC), maximum hypoglycemic response and time of maximum response (T(max)) were significantly higher (p < 0.001) when MH was administered in niosomal form compared to free drug solution. It could be concluded that MH-loaded niosome is promising extended-release preparation with better hypoglycemic efficiency.

docking studies were also performed to get better insights into the possible binding mode of the target compounds with VEGFR-2 active sites.

Recent studies demonstrated the role of antioxidants in preventing organ damage caused by free radicals. The present study was conducted to find out the modulatory effect of some antioxidants on lipid patterns in experimentally-induced liver damage. Rats chronically intoxicated with carbon tetrachloride (CCl4) were used as a model of liver injury terminating with fibrosis or cirrhosis. One hundred and sixty six albino rats were classified into five groups: one served as a control group; the second was subjected to oral administration of CCl4 (200 microL/100 g body weight) twice a week; the other three groups, in addition to CCl4, received oral doses of silymarin (30 mg/kg), vitamin E (200 IU/kg) and vitamin C (50 mg/kg) respectively. At the end of the experiment, the animals were killed, blood was collected and liver was taken for histopathological examination. Liver function tests, disturbed by CCl4 were significantly modulated by antioxidants, and histopathological examination showed that antioxidants ameliorated the necrotic and fibrotic changes caused by CCl4. Treatment with antioxidants was also shown to modulate the toxic effect of CCl4 on the lipid profile and malondialdehyde content. Administration of antioxidants could play an important role in prophylaxis against lipid peroxidation and consequently liver fibrosis caused by free radicals.

A new series of pyrimidine-5-carbonitrile derivatives has been designed as ATP mimicking tyrosine kinase inhibitors of the epidermal growth factor receptor (EGFR). These compounds were synthesized and evaluated for their in vitro cytotoxic activities against a panel of four human tumor cell lines, namely colorectal carcinoma (HCT-116), hepatocellular carcinoma (HepG-2), breast cancer (MCF-7), and non-small cell lung cancer cells (A549). Five of the synthesized compounds, 11a, 11b, 12b, 15b and 16a, were found to exhibit moderate antiproliferative activity against the tested cell lines and were more active than the EGFR inhibitor erlotinib. In particular, compound 11b showed 4.5- to 8.4-fold erlotinib activity against HCT-116, HepG-2, MCF-7, and A549 cells with IC50 values of 3.37, 3.04, 4.14, and 2.4 μM respectively. Moreover, the most cytotoxic compounds that showed promising IC50 values against the four cancer cell lines were subjected to further investigation for their kinase inhibitory activities against EGFRWT and EGFRT790M using homogeneous time resolved fluorescence (HTRF) assay. Compound 11b was also found to be the most active compound against both EGFRWT and mutant EGFRT790M, exhibiting IC50 values of 0.09 and 4.03 μM, respectively. The cell cycle and apoptosis analyses revealed that compound 11b can arrest the cell cycle at the G2/M phase and induce significant apoptotic effects in HCT-116, HepG-2, and MCF-7 cells. Additionally, compound 11b upregulated the level of caspase-3 by 6.5 fold in HepG-2 when compared with the control. Finally, molecular docking studies were carried out to examine the binding mode of the synthesized compounds against the proposed targets; EGFRWT and EGFRT790M. Additional in silico ADMET studies were performed to explore drug-likeness properties.

&lt;p&gt;&lt;em&gt;Abstrak&lt;/em&gt; - &lt;strong&gt;Perkembangan dunia perfilman saat ini sudah berkembang pesat, tak terkecuali di Indonesia.&lt;/strong&gt; &lt;strong&gt;Berbagai tema film telah diproduksi sebagai sarana hiburan maupun penyampaian pesan bagi khalayaknya.&lt;/strong&gt; &lt;strong&gt;Penelitian ini bertujuan mendeksipsikan pesan (&lt;em&gt;message&lt;/em&gt;) yang disampaikan dalam sebuah film dengan menganalisis isi (&lt;em&gt;content analysis&lt;/em&gt;) secara kualitatif dalan paparan cerita film “Nanti Kita Cerita Tentang Hari INI (NKCTHI)” yang bergenre drama keluarga yang telah mendeskripsikan tentang kedudukan dan peran seorang lelaki, suami dan ayah dalam sebuah keluarga yang digugat oleh anak-anaknya sesuai perkembangan jaman mereka. Pesan cerita film NKCTHI ini menggugat dominasi laki-laki sebagai suami dan sekaligus ayah dalam latar belakang masyarakat yang masih patriarki, dimana otoritas dan pusat kekuasaan masih dominan pada laki-laki. &lt;/strong&gt;&lt;/p&gt;&lt;p&gt;&lt;strong&gt;&lt;em&gt;Kata Kunci&lt;/em&gt;&lt;/strong&gt;– &lt;em&gt;film, analisis isi, kualitatif, komunikasi massa, media&lt;/em&gt;&lt;/p&gt;&lt;p&gt;&lt;em&gt;Abstract –&lt;/em&gt;&lt;strong&gt; Expanded growth in film industry all over the worlds, include Indonesia to released many theme and variant genre of movies for entertaintment and delivered messages for target audiences. The Objective of this study to describe about story message from family drama movie “&lt;em&gt;Nanti Kita Cerita Tentang Hari Ini (NKCTHI)&lt;/em&gt;”. This qualitative study used &lt;em&gt;content analysis&lt;/em&gt; method with description about role and position a man as husband and father in traditional society with patriarchy, when a man handled authority and power dominantly, who sued by his lovely children in family.&lt;/strong&gt;&lt;/p&gt;&lt;p&gt;&lt;strong&gt;&lt;em&gt;Keywords&lt;/em&gt;&lt;/strong&gt; – &lt;em&gt;film, content analysis, qualitative, mass communication, media&lt;/em&gt;&lt;/p&gt;