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Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting V600EBRAF

Abdel-Maksoud, Mohammed S.; Ali, Eslam M.H.; Ammar, Usama M.; Mersal, Karim I.; Yoo, Kyung Ho; Oh, Chang-Hyun


Mohammed S. Abdel-Maksoud

Eslam M.H. Ali

Karim I. Mersal

Kyung Ho Yoo

Chang-Hyun Oh


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 V600E B-RAF inhibitors, two series of pyrrolo[2,3-b]pyridine scaffold were designed and synthesized in attempt to develop new potent V600E B-RAF inhibitors. The 38 synthesized compounds were biologically evaluated for their V600E B-RAF inhibitory effect at single dose (10 μM). Compounds with high percent inhibition were tested to determine their IC 50 over V600E B-RAF. Compounds 34e and 35 showed the highest inhibitory effect with IC 50 values of 0.085 µM and 0.080 µM, 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.


Abdel-Maksoud, M. S., Ali, E. M., Ammar, U. M., Mersal, K. I., Yoo, K. H., & Oh, C. (2020). Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting V600EBRAF. Bioorganic and Medicinal Chemistry, 28(11), Article 115493.

Journal Article Type Article
Acceptance Date Apr 5, 2020
Online Publication Date Apr 10, 2020
Publication Date 2020-06
Deposit Date Dec 11, 2022
Journal Bioorganic & Medicinal Chemistry
Print ISSN 0968-0896
Publisher Elsevier
Peer Reviewed Peer Reviewed
Volume 28
Issue 11
Article Number 115493
Keywords B-RAF inhibitors, Kinase inhibitor, Anticancer, Pyrrolo[2,3-b]pyridine, SAR
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