(2S,2′R)-analogue of LG190178 is a major active isomer
(2S,2′R)-analogue of LG190178 is a major active isomer
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DOI：
10.1016/j.bmcl.2007.11.007
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发表时间：
2008-01-01
影响因子：
2.7
通讯作者：
Kurihara, Masaaki
中科院分区：
文献类型：
--
作者：
Hakamata, Wataru;Sato, Yukiko;Kurihara, Masaaki
维生素D受体（VDR）配体是用于治疗银屑病、骨质疏松症和继发性甲状旁腺功能亢进的治疗剂。VDR配体还显示出作为自身免疫性疾病和皮肤癌、前列腺癌、结肠癌和乳腺癌以及白血病的治疗剂的巨大潜力。LG 190178是一种新型的VDR非开环甾体配体。我们合成并评价了LG 190178的立体异构体，发现只有LG 190178的（2S，2 'R）-类似物（YR 301）具有强活性。(C)2007爱思唯尔有限公司保留所有权利。
Vitamin D receptor (VDR) ligands are therapeutic agents for the treatment of psoriasis, osteoporosis, and secondary hyperparathyroidism. VDR ligands also show immense potential as therapeutic agents for autoimmune diseases and cancers of the skin, prostate, colon, and breast as well as leukemia. LG190178 is a novel non-secosteroidal ligand for VDR. We synthesized and evaluated stereoisomers of LG190178 and found that only an (2S,2'R)-analogue of LG190178 (YR301) had strong activity. (C) 2007 Elsevier Ltd. All rights reserved.