Synthesis and biological evaluation of benzyl styrylsulfonyl derivatives as potent anticancer mitotic inhibitors

Osama Chahrour; Ashraf Abdalla; Frankie Lam; Carol Midgley; Shudong Wang

doi:10.1016/j.bmcl.2011.03.041

Synthesis and biological evaluation of benzyl styrylsulfonyl derivatives as potent anticancer mitotic inhibitors

Bioorg Med Chem Lett. 2011 May 15;21(10):3066-9. doi: 10.1016/j.bmcl.2011.03.041. Epub 2011 Mar 17.

Authors

Osama Chahrour¹, Ashraf Abdalla, Frankie Lam, Carol Midgley, Shudong Wang

Affiliation

¹ School of Pharmacy and Centre for Biomolecular Sciences, University of Nottingham, Nottingham NG7 2RD, UK.

PMID: 21463944
DOI: 10.1016/j.bmcl.2011.03.041

Abstract

We herein report the synthesis, biological activity and structure activity relationship of derivatives of benzylstyrylsulfone, benzylstyrylsulfine and benzylsulfonyl-N-phenylacetamide. A lead compound 7 represents a new class of mitotic inhibitors that demonstrates potent anti-proliferative activity and selectively induces cancer cell apoptosis while sparing non-transformed lung fibroblast.

Publication types

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

MeSH terms

Antimitotic Agents / chemical synthesis*
Antimitotic Agents / chemistry
Antimitotic Agents / pharmacology*
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Apoptosis / drug effects
Cell Line, Tumor
Humans
Structure-Activity Relationship
Styrenes / chemistry*
Sulfinic Acids / chemistry

Substances

Antimitotic Agents
Antineoplastic Agents
Styrenes
Sulfinic Acids
sulfonyl chloride