Synthesis and Cytotoxicity of 1-phenylethanolamine Carboxamide Derivatives: Effects on the Cell Cycle
Document Type
Article
Publication Date
12-2010
Publication Source
Medicinal Chemistry Research
Volume Number
19
Issue Number
9
First Page
1141
Last Page
1152
Publisher
Birkhauser Boston Inc.
ISSN
1054-2523
Abstract
Seven novel analogues of 1-phenylethanolamine carboxamide derivatives, 3a-3g, related to carboxamides isolated from Isodon excisus were synthesized and evaluated for their cytotoxic and apoptosis-induction properties against murine B16 and leukemia L1210 cell lines. Compounds containing no substitution at the 4'-position (3a-3d) or containing a 4'-amino (3e-3g) group were investigated. Generally, the amino-containing compounds were slightly more active than their unsubstituted congeners. Also, the indole-containing compounds 3c and 3f gave the strongest cytotoxic activity (IC50 = 25-87 mu M) against the growth of L1210 and B16 cancer cells. Compound 3f was subjected to flow cytometry studies and it was found to induce L1210 cells grown in culture to undergo apoptosis.
Recommended Citation
Published in: Medicinal Chemistry Research, Volume 19, Issue 9, December 1, 2010, pages 1141-1152. Copyright © 2010 Birkhauser Boston Inc., Cambridge, MA. The final published version is available at: http://dx.doi.org/10.1007/s00044-009-9258-9