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Bioorg Med Chem Lett. 2011 Nov 1;21(21):6310-3. doi: 10.1016/j.bmcl.2011.08.118. Epub 2011 Sep 1.

Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: structural requirements for better physicochemical and biological properties.

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Central Research Laboratories, Kaken Pharmaceutical Co., Ltd 14, Shinomiya Minamikawara-cho, Yamashina, Kyoto 607-8042, Japan.


A rationally designed tetrahydroquinoline (1) for nonsteroidal selective androgen receptor modulators was modified for the exploration of promising compounds by Grieco three-component condensation using various dienophiles. Based on the in vitro effects and physicochemical properties of the synthesized compounds, compound 4c was selected for further study. Compound 4c increased the femoral bone mineral density as much as DHT, but it reduced the uterus effect compared with DHT in ovariectomized rats. Thus, compound 4c has desirable osteoanabolic effects with weak undesirable effects on the uterus in a female osteoporosis model.

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