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Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors |
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| Authors: | Steven D Fidanze Dachun Liu Robert A Mantei Lisa A Hasvold John K Pratt George S Sheppard Le Wang James H Holms Yujia Dai Ana Aguirre Andrew Bogdan Justin D Dietrich Jasmina Marjanovic Chang H Park Charles W Hutchins Xiaoyu Lin Mai H Bui Xiaoli Huang Keith F McDaniel |
| Institution: | 1. AbbVie Inc., 1 North Waukegan Rd., North Chicago, IL 60064, United States |
| 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-pyrrolo2,3-c]pyridin-7(6H)-ones (A) and the 1-methyl-1H-pyrrolo2,3-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. |
| Keywords: | Corresponding authors |
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