香豆素类化合物作为新型 17β-羟甾类脱氢酶 3 型抑制剂，有望用于治疗前列腺癌。
Coumarins as novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer.
机构信息
Environmental Health Science Laboratory, Sumitomo Chemical Co., Ltd, 1-98, Kasugadenaka 3-chome, Konohana-ku, Osaka 554-8558, Japan.
出版信息
Bioorg Med Chem Lett. 2010 Jan 1;20(1):272-5. doi: 10.1016/j.bmcl.2009.10.111. Epub 2009 Nov 10.
PMID:19954971
Abstract
The synthesis and SAR studies of 3- and 4-substituted 7-hydroxycoumarins as novel 17beta-HSD3 inhibitors are discussed. The most potent compounds from this series exhibited low nanomolar inhibitory activity with acceptable selectivity versus other 17beta-HSD isoenzymes and nuclear receptors.
摘要
讨论了新型 17β-HSD3 抑制剂 3-和 4-取代 7-羟基香豆素的合成和 SAR 研究。该系列中最有效的化合物对其他 17β-HSD 同工酶和核受体具有可接受的选择性，表现出低纳摩尔的抑制活性。
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