Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities

Shinnosuke Hosoda; Aya Tanatani; Ken-ichi Wakabayashi; Yusuke Nakano; Hiroyuki Miyachi; Kazuo Nagasawa; Yuichi Hashimoto

doi:10.1016/j.bmcl.2005.06.044

Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4327-31. doi: 10.1016/j.bmcl.2005.06.044.

Authors

Shinnosuke Hosoda¹, Aya Tanatani, Ken-ichi Wakabayashi, Yusuke Nakano, Hiroyuki Miyachi, Kazuo Nagasawa, Yuichi Hashimoto

Affiliation

¹ Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.

PMID: 16019211
DOI: 10.1016/j.bmcl.2005.06.044

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Androgen Antagonists / chemical synthesis*
Androgen Antagonists / pharmacology
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology
Benzene Derivatives / chemical synthesis
Benzene Derivatives / pharmacology
Cell Differentiation / drug effects
Cell Proliferation / drug effects
Cholecalciferol / agonists*
Dose-Response Relationship, Drug
HL-60 Cells
Humans
Ligands
Structure-Activity Relationship
Testosterone / pharmacology

Substances

Androgen Antagonists
Antineoplastic Agents
Benzene Derivatives
Ligands
Cholecalciferol
Testosterone