設計合成和評估用於治療前列腺癌的CBP溴結構域抑製劑。PK評估、肝微粒體穩定性測定和Caco-2滲透性測定通過hjc黄金城進行

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.