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Synthesis and Structure−Activity Relationship of 2-Aminobenzophenone Derivatives as Antimitotic Agents

Authors :
Liou, J.-P.
Chang, C.-W.
Song, J.-S.
Yang, Y.-N.
Yeh, C.-F.
Tseng, H.-Y.
Lo, Y.-K.
Chang, Y.-L.
Chang, C.-M.
Hsieh, H.-P.
Source :
Journal of Medicinal Chemistry; June 2002, Vol. 45 Issue: 12 p2556-2562, 7p
Publication Year :
2002

Abstract

A new type of inhibitor of tubulin polymerization was discovered on the basis of the combretastatin molecular skeleton. The lead compounds in this series, compounds <BO>6</BO> and <BO>7</BO>, strongly inhibited tubulin polymerization in vitro and significantly arrested cells at the G<INF>2</INF>/M phase. Compounds <BO>6</BO> and <BO>7</BO> yielded 50- to 100-fold lower IC<INF>50</INF> values than did combretastatin A-4 against Colo 205, NUGC3, and HA22T human cancer cell lines as well as similar or greater growth inhibitory activities than did combretastain A-4 against DLD-1, HR, MCF-7, DU145, HONE-1, and MES-SA/DX5 human cancer cell lines. Structure−activity relationship information revealed that introduction of an amino group at the ortho position of the benzophenone ring plays an integral role for increased growth inhibition.

Details

Language :
English
ISSN :
00222623 and 15204804
Volume :
45
Issue :
12
Database :
Supplemental Index
Journal :
Journal of Medicinal Chemistry
Publication Type :
Periodical
Accession number :
ejs2247870
Full Text :
https://doi.org/10.1021/jm010365+