Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors

DOI: 10.1016/j.bmcl.2018.04.020

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1804 - 1810 (2018)

Update date:2022-07-30

Topics:

Authors:

Fidanze, Steven D.

Liu, Dachun

Mantei, Robert A.

Hasvold, Lisa A.

Pratt, John K.

Sheppard, George S.

Wang, Le

Holms, James H.

Dai, Yujia

Aguirre, Ana

Bogdan, Andrew

Dietrich, Justin D.

Marjanovic, Jasmina

Park, Chang H.

Hutchins, Charles W.

Lin, Xiaoyu

Bui, Mai H.

Huang, Xiaoli

Wilcox, Denise

Li, Leiming

Wang, Rongqi

Kovar, Peter

Magoc, Terrance J.

Rajaraman, Ganesh

Albert, Daniel H.

Shen, Yu

Kati, Warren M.

McDaniel, Keith F.

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Article abstract of DOI:10.1016/j.bmcl.2018.04.020

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

Full text of DOI:10.1016/j.bmcl.2018.04.020

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Product name:4-{2-[(cyclopropylmethyl)amino]phenyl}-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one

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