具有双维生素D3激动和雄激素拮抗活性的配体。
Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities.
作者信息
Hosoda Shinnosuke, Tanatani Aya, Wakabayashi Ken-ichi, Nakano Yusuke, Miyachi Hiroyuki, Nagasawa Kazuo, Hashimoto Yuichi
机构信息
Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
出版信息
Bioorg Med Chem Lett. 2005 Oct 1;15(19):4327-31. doi: 10.1016/j.bmcl.2005.06.044.
Ligands possessing dual vitamin D3-agonistic (estimated as HL-60 monocytic cell differentiation induction) and androgen-antagonistic (estimated as testosterone-induced SC-3 cell growth inhibition) activities with various activity spectra were prepared based on a substituted bis-phenylmethane skeleton. Some of them were revealed to be potent androgen antagonists with a nonsecosteroidal vitamin D3 skeleton.
基于取代双苯甲烷骨架制备了具有不同活性谱的配体，这些配体具有双重维生素D3激动活性（以HL-60单核细胞分化诱导来评估）和雄激素拮抗活性（以睾酮诱导的SC-3细胞生长抑制来评估）。其中一些被发现是具有非甾体维生素D3骨架的强效雄激素拮抗剂。
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