Synthesis, characterization and biological evaluation of some 16β-azolyl-3β-amino-5α-androstane derivatives as potential anticancer agents

Hao Guo; Guolan Zhang; Tao Zhang; Xianran He; Zhongyuan Wu; Yuling Xiao; Yuanhu Pan; Guofu Qiu; Peng Liu; Xianming Hu

doi:10.1016/j.ejmech.2011.05.030

Synthesis, characterization and biological evaluation of some 16β-azolyl-3β-amino-5α-androstane derivatives as potential anticancer agents

Eur J Med Chem. 2011 Sep;46(9):3662-74. doi: 10.1016/j.ejmech.2011.05.030. Epub 2011 May 23.

Authors

Hao Guo¹, Guolan Zhang, Tao Zhang, Xianran He, Zhongyuan Wu, Yuling Xiao, Yuanhu Pan, Guofu Qiu, Peng Liu, Xianming Hu

Affiliation

¹ State Key Laboratory of Virology, Ministry of Education Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Science, Wuhan 430071, China.

PMID: 21641694
DOI: 10.1016/j.ejmech.2011.05.030

Abstract

A series of new 16β-azolyl-3β-amino-5α-androstane derivatives were synthesized and characterized. The new compounds were screened for their anticancer activity against the human cancer cell lines SW480, A549, HepG2, HeLa and SiHa in vitro using the MTT assay. The results of the in vitro study showed that a number of compounds have shown IC(50) values lower than 20 μM against the five cancer cell lines.

Publication types

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

MeSH terms

Androstanes / chemical synthesis*
Androstanes / chemistry
Androstanes / pharmacology*
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Benzimidazoles / chemical synthesis*
Benzimidazoles / chemistry
Benzimidazoles / pharmacology*
Cell Line, Tumor
Crystallography, X-Ray
Drug Screening Assays, Antitumor
Humans
Inhibitory Concentration 50
Magnetic Resonance Spectroscopy
Models, Molecular
Triazoles / chemical synthesis*
Triazoles / chemistry
Triazoles / pharmacology*

Substances

Androstanes
Antineoplastic Agents
Benzimidazoles
Triazoles