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Copyright of Medical Journal of Viral Hepatitis is the property of Egyptian Liver Research Institute & Hospital (ELRISH) and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

The present work aimed to synthesize different substituted glycinamide derivatives. A series of novel substituted 2-((N-benzyl-5-bromo-2-methoxyphenyl) sulfonamide) and their glycinamide derivatives (5a–5p) were synthesized. We developed a simple strategy for synthesizing functionally diverse sulfonamide and glycinamide derivatives through a series of steps. A series of molecules containing amide derivatives were designed and synthesized, and their structures were elucidated and confirmed by1H NMR, 13 C NMR, LCMS, and their purity was checked using HPLC. The synthesized compounds were screened for anticancer activity against A-549 and A431 cancer cell lines by MTT assay and then docking studies were carried out to understand the molecular interactions. The preliminary bioassay suggests that most compounds showed remarkable anti-proliferation activity. Gefitinib was used as a positive control. The compounds 5g and 5f were active compared with Gefitinib in both the cell lines. [ABSTRACT FROM AUTHOR]

A series of novel imidazo[1,2‐b]pyridazin‐3‐yl acetamide derivatives (9a‐9j) were synthesized from a 3,6‐dichloropyridazine. We have developed a simple strategy for the synthesis of functionally diverse imidazole, and pyridiazine derivatives were reported via a series of steps. The work involves bicyclic imidazo‐pyridazine ring formation, halogenation, cynation, hydrolysis, peptide coupling, and Buchwald reaction. The structure of the synthesized compounds was confirmed by IR, 1H NMR, 13C NMR,19F NMR, mass spectra, and elemental analysis, and purity is checked by HPLC. All synthesized compounds were screened for anticancer activity against A‐549 and Du‐145 cancer cell lines by MTT assay. The preliminary bioassay suggests that most of the compounds show anti‐proliferation with different degrees; doxorubicin was used as positive control. The synthesized compound shows IC50 values in the range of 1.74μM to 16.17μM in both cell lines. The compounds 9e, 9g, and 9h were active compared with doxorubicin in both the cell lines. The compounds having cyclopentyl ring are active compared with higher and lower carbon analogues. [ABSTRACT FROM AUTHOR]

A series of novel thiazol‐2‐yl substituted‐1‐sulfonamide derivatives were synthesized from anilines. This involved the coupling of sulfonyl chlorides with thiazol amine to obtain the final compounds 7a–7j and 8a–8j. All synthesized compounds were screened for anticancer activity against MCF‐7, HeLa, A‐549, and Du‐145 cancer cell lines by 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) assay. Preliminary bioassay suggests that most of the compounds show anti‐proliferation to different degrees, with doxorubicin used as positive control. The synthesized compounds show IC50 values in the range 2.74–8.17 μM in the different cell lines. The compounds 7d, 7e, 8a, 8d, and 8e were active compared to doxorubicin. The compounds having butyl and pantyl chains were more active than their lower and higher carbon chains and also their ring counterparts. Novel thiazol‐2‐yl substituted‐1‐sulfonamide derivatives were synthesized and identified for their anticancer activity against MCF‐7, HeLa, A‐549 and Du‐145 cancer cell lines by 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide assay. The synthesized compound shows IC50 values in the range of 2.74‐8.17 µM in different cell lines. The compounds having butyl and pantyl chains were active compared with their lower and higher carbon chains and also with their ring counterparts. [ABSTRACT FROM AUTHOR]

A series of novel N‐(2‐(pyridine‐4‐yl)‐1H‐pyrrolo[3,2‐c]‐pyridin‐6‐yl‐(substituted)‐sulfonamide derivatives were synthesized from 2‐bromo‐6‐nitro‐1H‐pyrrolo[3,2‐c]pyridine through a series of reactions including Suzuki reaction, reduction, protection, and sulfonamide coupling. All the synthesized compounds were screened for anticancer activity against MCF‐7, HeLa, A‐549, and Du‐145 cancer cell lines by the MTT assay. The preliminary bioassay suggests that most of the compounds show antiproliferation with different degrees. Doxorubicin was used as a positive control. Among the synthesized compounds, 8d and 8h were most active compared with the standard in cell line data. The synthesized compounds 8d and 8h show IC50 values in the range of 1.88–5.16 μM for all the cell lines. Compounds 8d and 8h were further studied for a panel of eight human kinase at 10 μM concentrations and the result shows 64% to 70% inhibitions for both Aurora‐A and Aurora‐B kinase. [ABSTRACT FROM AUTHOR]

AbstractThis study investigates the drug-like properties of target molecules containing thiophene sulfonamide groups (7a–7s) using computational molecular docking techniques. The binding interactions of these derivatives were assessed using protein 2NSD (Enoyl acyl carrier protein reductase InhA, complexed with N-(4-methylbenzoyl)-4-benzylpiperidine, PDB DOI: 10.2210/pdb2NSD/pdb) as the receptor. Molecular docking results revealed notable docking scores for all compounds, ranging from −6 to −12 kcal/mol. Compounds 7e, 7i, and 7f, in particular, demonstrated impressive glide scores (>11 kcal/mol) and were selected for further analysis through molecular dynamics simulations, which provided deeper insights into their dynamic behavior and stability. The drug-like properties of these molecules were evaluated based on Lipinski’s Rule of Five and ADME (Absorption, Distribution, Metabolism, and Excretion) criteria and compared with known drugs. Additionally, we synthesized these target molecules (7a–7s) using Suzuki-Miyaura coupling with a nickel catalyst replacing palladium. The chemical structures of the synthesized compounds were confirmed through elemental analysis, LC-MS,1H-NMR, and 13C-NMR spectroscopy. [ABSTRACT FROM AUTHOR]