Abdel-Maksouda, Mohammed S. Ammar, Usama M. Oh, Chang-Hyun 2024-01-19T20:02:32Z 2024-01-19T20:02:32Z 2022-01-10 2019-05-15 0968-0896 https://pubs.kist.re.kr/handle/201004/119987 In this work, a new series of imidazo[2,1-b]thiazole was designed and synthesized. The new compounds are having 3-fluorophenyl at position 6 of imidazo[2,1-b]thiazole and pyrimidine ring at position 5. The pyrimidine ring containing either amide or sulphonamide moiety attached to a linker (ethyl or propyl) at position 2 of the pyrimidine ring. The final compounds were selected by NCI for in vitro cytotoxicity screening. Most derivatives showed cytotoxic activity against colon cancer and melanoma cell lines. In addition, IC(50)s of the target compounds were determined over A375 and SK-MEL-28 cell lines using sorafenib as positive control. Compounds12b, 12c, 12e, 12f, 15a, 15d, 15f, 14g and 15h exhibited superior activity when compared to sorafenib. The most potent compounds were tested against wild type BRAF, v600e BRAF, and CRAF. Compound 15h exhibited a potential inhibitory effect against(V600E)BRAF (IC50 = 9.3 nM). English PERGAMON-ELSEVIER SCIENCE LTD SIGNALING PATHWAYS CANCER DESIGN KINASE RESISTANCE SURVIVAL AGENTS IDENTIFICATION PROLIFERATION DERIVATIVES Anticancer profile of newly synthesized BRAF inhibitors possess 5-(pyrimidin-4-yl)imidazo[2,1-b]thiazole scaffold Article 10.1016/j.bmc.2019.03.062 1 BIOORGANIC & MEDICINAL CHEMISTRY, v.27, no.10, pp.2041 - 2051 BIOORGANIC & MEDICINAL CHEMISTRY 27 10 2041 2051 scie scopus 000465176600010 2-s2.0-85063762481 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article SIGNALING PATHWAYS CANCER DESIGN KINASE RESISTANCE SURVIVAL AGENTS IDENTIFICATION PROLIFERATION DERIVATIVES Imidazo[2,1-b]thiazole Anticancer Colon cancer Melanoma BAF inhibitors