Synthesis, biological evaluation and molecular docking of 4-Amino-2H-benzohchromen-2-one (ABO) analogs containing the piperazine moiety.

Synthesis, biological evaluation and molecular docking of 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs containing the piperazine moiety. Bioorg Med Chem. 2019 Aug 28;:115081 Authors: Chen H, Zhang J, Hu P, Qian Y, Li J, Shen J Abstract Prostate cancer (PCa) is a major cause of cancer-related male death in worldwide. To develop of potential anti-prostate cancer agents, 22 kinds of 4-Amino-2H-benzo[h]chromen-2-one analogs were designed and synthesized as potent androgen receptor (AR) antagonist through rational drug modification leading to the discovery of a series of novel antiproliferative compounds. Analogs (3, 4, 5, 7, 8, 10, 11, 12, 16, 18, 21, 23, and 24) exhibited potent antagonistic potency against AR (inhibition>50%), and exhibited potent AR binding affinities as well as displayed the higher activities than finasteride toward LNCaP cells (AR-rich) versus PC-3 cells (AR-deficient). Moreover, the docking study suggested that the most potent antagonist 23 mainly bind to AR ligand binding pocket (LBP) site through Van der Waals' force interactions. The structure-activity relationship (SAR) of these designed 4-Amino-2H-benzo[h]chromen-2-one analogs was rationally explored and discussed. Collectively, this work provides a potential lead compound for anticancer agent development related to prostate cancer therapy, and took a step forward towards the development of novel and improved AR antagonists. PMID: 31493989 [PubMed - as supplied by publis...
Source: Bioorganic and Medicinal Chemistry - Category: Chemistry Authors: Tags: Bioorg Med Chem Source Type: research

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(Society of Nuclear Medicine and Molecular Imaging) Researchers have discovered a new way to optimize results in treating patients with prostate cancer tumors while minimizing negative side effects. The study is featured in the November issue of The Journal of Nuclear Medicine.
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