合成含五氟硫基（SF ）部分的雄激素受体拮抗剂。
Synthesis of androgen receptor antagonists containing a pentafluorosulfanyl (SF ) moiety.
机构信息
Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, P. R. China.
The National Center for Drug Screening and the CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences (CAS), Shanghai, P. R. China.
出版信息
Arch Pharm (Weinheim). 2018 Nov;351(11):e1800175. doi: 10.1002/ardp.201800175. Epub 2018 Oct 15.
A novel scaffold of pentafluorosulfanyl (SF )-containing enzalutamide analogues was discovered for potent androgen receptor (AR) antagonists through rational drug design. Several compounds showed good biological profiles in AR binding. Of the derivatives studied, compound 8a had potent AR antagonist activity (IC = 7.1 ± 1.0 µM) and high efficacy (104.5 ± 12.8%). It exhibited an inhibitory effect comparable to that of enzalutamide (inhibition = 66.0 and 77.9%, respectively) in a prostate cancer cell line. The results point to the potential of using this scaffold to develop new AR antagonists.
通过合理的药物设计，发现了一种含五氟硫基（SF）的恩扎卢胺类似物的新型支架，作为有效的雄激素受体（AR）拮抗剂。几种化合物在 AR 结合方面表现出良好的生物学特性。在所研究的衍生物中，化合物 8a 具有很强的 AR 拮抗剂活性（IC = 7.1 ± 1.0 µM）和高效性（104.5 ± 12.8%）。在前列腺癌细胞系中，它表现出与恩扎卢胺相当的抑制作用（分别为 66.0%和 77.9%）。这些结果表明，该支架有可能用于开发新的 AR 拮抗剂。
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