Laboratory of Translational Therapeutics, Pharmacology Research Center, Division of Drug Discovery Research, Korea Research Institute of Chemical Technology, P.O. Box 107, Yuseong-gu, Daejeon 305-600, Republic of Korea.
Bioorg Med Chem Lett. 2013 Jul 1;23(13):3887-90. doi: 10.1016/j.bmcl.2013.04.065. Epub 2013 May 3.
In this study, we synthesized the BF-3 binding small molecules, a series of pyridazinone-based compounds, as a novel class of non-LBP antiandrogens for treating prostate cancer by inhibiting androgen receptor. The new class compound was discovered to inhibitor the viability of AR-dependent human prostate LNCap cells and AR activity combining with the computational method. It showed a good physicochemical and PK property.
在这项研究中，我们合成了 BF-3 结合小分子，即一系列基于哒嗪酮的化合物，作为一类新型的非 LBP 抗雄激素药物，通过抑制雄激素受体来治疗前列腺癌。通过计算方法发现，新型化合物能够抑制 AR 依赖性人前列腺 LNCap 细胞的活力和 AR 活性。它表现出良好的理化和 PK 性质。
