Abstract
Chiral derivatives of two cyclohexylethyl halopyridyl thiourea compounds (HI-509 and HI-510), two α -methyl benzyl halopyridyl compounds (HI-511 and HI-512), and a cyclohexyl ethyl thiazolyl thiourea compound (HI-513) were synthesized and evaluated for their anti-cancer activity. Preliminary screening indicated that the (S)- isomers displayed improved activity in comparison with (R)- enantiomers to inhibit tubulin polymerization and activate caspase- 3. In accordance with these results, the thiourea derivatives displayed potent anti-cancer activity against human B-lineage (Nalm-6) and T-lineage (Molt-3) acute lymphoblastic leukemia cell lines. Based on the results we conclude that the anti-leukemic activity of these compounds also depends on their chirality.
Keywords: Stereochemistry, Thiourea, Zebrafish, Caspase, Leukemia
Letters in Drug Design & Discovery
Title: Stereochemistry as a Determinant of the Anti-Leukemic Potency of Halopyridyl and Thiazolyl Thiourea Compounds
Volume: 4 Issue: 5
Author(s): Taracad K. Venkatachalam, Alexi O. Vassilev, Alexi Benyunov, Olga O. Grigoriants, Heather E. Tibbles and Fatih M. Uckun
Affiliation:
Keywords: Stereochemistry, Thiourea, Zebrafish, Caspase, Leukemia
Abstract: Chiral derivatives of two cyclohexylethyl halopyridyl thiourea compounds (HI-509 and HI-510), two α -methyl benzyl halopyridyl compounds (HI-511 and HI-512), and a cyclohexyl ethyl thiazolyl thiourea compound (HI-513) were synthesized and evaluated for their anti-cancer activity. Preliminary screening indicated that the (S)- isomers displayed improved activity in comparison with (R)- enantiomers to inhibit tubulin polymerization and activate caspase- 3. In accordance with these results, the thiourea derivatives displayed potent anti-cancer activity against human B-lineage (Nalm-6) and T-lineage (Molt-3) acute lymphoblastic leukemia cell lines. Based on the results we conclude that the anti-leukemic activity of these compounds also depends on their chirality.
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Venkatachalam K. Taracad, Vassilev O. Alexi, Benyunov Alexi, Grigoriants O. Olga, Tibbles E. Heather and Uckun M. Fatih, Stereochemistry as a Determinant of the Anti-Leukemic Potency of Halopyridyl and Thiazolyl Thiourea Compounds, Letters in Drug Design & Discovery 2007; 4 (5) . https://dx.doi.org/10.2174/157018007780867870
DOI https://dx.doi.org/10.2174/157018007780867870 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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