Synthesis and SAR study of diphenylbutylpiperidines as cell autophagy inducers

Gang Chen; Hongguang Xia; Yu Cai; Dawei Ma; Junying Yuan; Chengye Yuan

doi:10.1016/j.bmcl.2010.11.029

Synthesis and SAR study of diphenylbutylpiperidines as cell autophagy inducers

Bioorg Med Chem Lett. 2011 Jan 1;21(1):234-9. doi: 10.1016/j.bmcl.2010.11.029. Epub 2010 Nov 11.

Authors

Gang Chen¹, Hongguang Xia, Yu Cai, Dawei Ma, Junying Yuan, Chengye Yuan

Affiliation

¹ State Key Laboratory of Bio-organic and Natural Product Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China.

PMID: 21126871
DOI: 10.1016/j.bmcl.2010.11.029

Abstract

A novel series of diphenylbutylpiperidines as autophagy inducers was described and extensive SAR studies resulted in derivatives (15d-e, 15i-j) with 10-fold greater activity than the lead compounds 1 and 2. Meanwhile, a new synthetic route to diphenylbutyl bromide (6) from bromobenzene and γ-butyrolactone was also reported here.

Publication types

Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't

MeSH terms

Autophagy*
Cell Line, Tumor
Humans
Piperidines / chemical synthesis
Piperidines / chemistry*
Piperidines / pharmacology
Structure-Activity Relationship

Substances

Piperidines
piperidine