Authors Abdel-Maksoud, MS; Ali, EMH; Ammar, UM; Mersal, KI; Yoo, KH; Oh, CH in PERGAMON-ELSEVIER SCIENCE LTD published article about BRAF MUTATIONS; SIGNALING PATHWAY; RAF KINASE; MULTIKINASE INHIBITOR; MAPK PATHWAY; MELANOMA; MUTANT; SENSITIVITY; ACTIVATION; SORAFENIB in [Abdel-Maksoud, Mohammed S.] Natl Res Ctr NRC ID 60014618, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Giza 12622, Egypt; [Ali, Eslam M. H.; Ammar, Usama M.; Mersal, Karim I.; Oh, Chang-Hyun] KIST Sch, Korea Inst Sci & Technol, Ctr Biomat, Seoul 02792, South Korea; [Ali, Eslam M. H.; Ammar, Usama M.; Mersal, Karim I.; Oh, Chang-Hyun] Univ Sci & Technol UST, Daejeon 34113, South Korea; [Ali, Eslam M. H.] Modern Univ Technol & Informat MTI, Pharmaceut Chem Dept, Fac Pharm, Cairo 12055, Egypt; [Ammar, Usama M.] Ahram Canadian Univ, Pharmaceut Chem Dept, Fac Pharm, Giza 12566, Egypt; [Yoo, Kyung Ho] Korea Inst Sci & Technol, Chem Kinom Res Ctr, Seoul, South Korea in 2020, Cited 37. Category: isothiazole. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2
Several pyrrolo[2,3-b]pyridine-based B-RAF inhibitors are well known and some of them are currently FDA approved as anticancer agents. Based on the structure of these FDA approved B-V600E-RAF inhibitors, two series of pyrrolo[2,3-b]pyridine scaffold were designed and synthesized in attempt to develop new potent B-V600E-RAF inhibitors. The 38 synthesized compounds were biologically evaluated for their B-V600E-RAF inhibitory effect at single dose (10 mu M). Compounds with high percent inhibition were tested to determine their IC50 over (V600E)BRAF. Compounds 34e and 35 showed the highest inhibitory effect with IC50 values of 0.085 mu M and 0.080 mu M, respectively. Headed for excessive biological evaluation, the synthesized derivatives were tested over sixty diverse human cancer cell lines. Only compound 35 emerged as a potent cytotoxic agent against different panel of human cancer cell lines.
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Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com