2. Academic Validation
  3. Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors

  • Bioorg Med Chem Lett. 2018 Jun 1;28(10):1804-1810. doi: 10.1016/j.bmcl.2018.04.020.
Steven D Fidanze 1,  Dachun Liu 2,  Robert A Mantei 3,  Lisa A Hasvold 3,  John K Pratt 3,  George S Sheppard 3,  Le Wang 3,  James H Holms 3,  Yujia Dai 3,  Ana Aguirre 3,  Andrew Bogdan 3,  Justin D Dietrich 3,  Jasmina Marjanovic 3,  Chang H Park 3,  Charles W Hutchins 3,  Xiaoyu Lin 3,  Mai H Bui 3,  Xiaoli Huang 3,  Denise Wilcox 3,  Leiming Li 3,  Rongqi Wang 3,  Peter Kovar 3,  Terrance J Magoc 3,  Ganesh Rajaraman 3,  Daniel H Albert 3,  Yu Shen 3,  Warren M Kati 3,  Keith F McDaniel 3
Affiliations

Affiliations

  • 1 AbbVie Inc., 1 North Waukegan Rd., North Chicago, IL 60064, United States. Electronic address: steve.fidanze@abbvie.com.
  • 2 AbbVie Inc., 1 North Waukegan Rd., North Chicago, IL 60064, United States. Electronic address: dachun.liu@abbvie.com.
  • 3 AbbVie Inc., 1 North Waukegan Rd., North Chicago, IL 60064, United States.
PMID: 29678460 DOI: 10.1016/j.bmcl.2018.04.020
Abstract

Novel conformationally constrained BET bromodomain inhibitors have been developed. These inhibitors were optimized in two similar, yet distinct chemical series, the 6-methyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-ones (A) and the 1-methyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-ones (B). Each series demonstrated excellent activity in binding and cellular assays, and lead compounds from each series demonstrated significant efficacy in in vivo tumor xenograft models.

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