Design, Synthesis, and Biological Evaluations of 2,5-Diaryl-2,3-dihydro-1,3,4-oxadiazoline Analogs of Combretastatin-A4

Authors

Lauren Lee, Hope CollegeFollow
Lyda M. Robb, University of Texas at San Antonio
Megan Lee, Hope CollegeFollow
Ryan Davis, Hope College
Hilary Mackay, Hope College
Sameer Chavda, Hope College
Balaji Babu, Hope College
Erin L. O'Brien, University of Texas at San Antonio
April L. Risinger, University of Texas at San Antonio
Susan L. Mooberry, University of Texas at San Antonio
Moses Lee, Hope CollegeFollow

Document Type

Article

Publication Date

1-14-2010

Publication Source

Journal of Medicinal Chemistry

Volume Number

53

Issue Number

1

First Page

325

Last Page

334

Publisher

American Chemical Society

ISSN

0022-2623

Abstract

A total of 24 novel 2,5-diaryl-1,3,4-oxadiazoline analogs of combretastatin A-4 (CA-4, 1) were designed, synthesized, and evaluated for biological activities. The compounds represent two structural classes; the Type I class has three methoxy groups on the A ring and the Type I I class hits a single methoxy group on the A ring. Biological evaluations demonstrate that multiple structural features control the biological potency. Four of the compounds,

Recommended Citation

Published in: Journal of Medicinal Chemistry, Volume 53, Issue 1, January 14, 2010, pages 325-334. Copyright © 2010 American Chemical Society, Washington D.C.. The final published version is available at: http://dx.doi.org/10.1021/jm901268n