Abdel-Maksoud, Mohammed S. El-Gamal, Mohammed I. El-Din, Mahmoud M. Gamal Oh, Chang Hyun 2024-01-19T21:02:26Z 2024-01-19T21:02:26Z 2022-01-10 2019-01-01 1475-6366 https://pubs.kist.re.kr/handle/201004/120481 The present work describes the design and synthesis of a novel series of 1,3-diaryl-4-sulfonamidoarylpyrazole derivatives 1a-q and 2a-q and their in vitro biological activities. The target compounds were evaluated for antiproliferative activity against NCI-60 cell line panel. Compounds 1c, 1g, 1k-m, 1o, 2g, 2h, 2k-m, 2o, and 2q showed the highest mean inhibition percentages at 10 mu M single-dose testing and were selected to be tested at 5-dose mode. The ICs50 of the most potent compounds were determined over the 60 cell lines. Compound 2l exhibited the strongest activity against different cell lines with IC50 0.33 mu M against A498 renal cancer cell line. Compound 2l was tested over a panel of 20 kinases to determine its molecular target(s), and its IC50 values over the most sensitive kinases were defined. In vitro stability and in vivo pharmacokinetic profile of compound 2l was also investigated. English TAYLOR & FRANCIS LTD MELANOMA-CELL LINE ANTIPROLIFERATIVE ACTIVITY RAF KINASE CANCER DIARYLAMIDES DIARYLUREAS SCAFFOLD SERIES Design, synthesis, in vitro anticancer evaluation, kinase inhibitory effects, and pharmacokinetic profile of new 1,3,4-triarylpyrazole derivatives possessing terminal sulfonamide moiety Article 10.1080/14756366.2018.1530225 1 JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, v.34, no.1, pp.97 - 109 JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 34 1 97 109 scie scopus 000448446300001 2-s2.0-85055412577 Biochemistry & Molecular Biology Chemistry, Medicinal Biochemistry & Molecular Biology Pharmacology & Pharmacy Article MELANOMA-CELL LINE ANTIPROLIFERATIVE ACTIVITY RAF KINASE CANCER DIARYLAMIDES DIARYLUREAS SCAFFOLD SERIES Anticancer kinase inhibitor pharmacokinetic pyrazole sulfonamide