Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting v600EBRAF

Title
Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting v600EBRAF
Authors
유경호오창현호스니 알리마그디 아마르카림 이브라힘 메르살Mohammed S. Abdel-Maksoud
Keywords
B-Raf inhibitors; Kinase inhibitor; Anticancer; pyrrolo[2,3-b]pyridine; SAR
Issue Date
2020-06
Publisher
Bioorganic & medicinal chemistry
Citation
VOL 28-115507
Abstract
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 V600EB-RAF inhibitors, two series of pyrrolo[2,3-b]pyridine scaffold were designed and synthesized in attempt to develop new potent V600EB-RAF inhibitors. The 38 synthesized compounds were biologically evaluated for their V600EB-RAF inhibitory effect at single dose (10 μM). Compounds with high percent inhibition were tested to determine their IC50 over V600EB-RAF. Compounds 34e and 35 showed the highest inhibitory effect with IC50 values of 0.085 µ M and 0.080 µ 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.
URI
http://pubs.kist.re.kr/handle/201004/71695
ISSN
0968-0896
Appears in Collections:
KIST Publication > Article
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