Design, synthesis, and biological evaluation of CBP bromodomain inhibitors for the treatment of prostate cancer. PK evaluation, liver microsomal stability assay, and Caco-2 permeability assay were performed at Medicilon

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Design, synthesis, and biological evaluation of CBP bromodomain inhibitors for the treatment of prostate cancer. PK evaluation, liver microsomal stability assay, and Caco-2 permeability assay were performed at Medicilon

2023-07-11

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Prostate cancer (PCa) is one of the most commonly diagnosed cancers and the leading cause of cancer mortalities in men. CREB (cyclic-AMP responsive element binding protein) binding protein (CBP) is a potential target for prostate cancer treatment. Researchers designed 1-(Indolizin-3-yl)ethan-1-ones as CBP bromodomain inhibitors for the treatment of prostate cancer.

Pharmacokinetic properties evaluation were analyzed by Medicilon.

Liver microsomal stability assay were performed at Medicilon.

Caco-2 permeability assay was analyzed by Medicilon.

Reference:

Qiuping Xiang, et al. Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer. J Med Chem. 2022 Jan 13;65(1):785-810. doi: 10.1021/acs.jmedchem.1c01864.