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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Stereochemistry as a Determinant of the Anti-Leukemic Potency of Halopyridyl and Thiazolyl Thiourea Compounds

Author(s): Taracad K. Venkatachalam, Alexi O. Vassilev, Alexi Benyunov, Olga O. Grigoriants, Heather E. Tibbles and Fatih M. Uckun

Volume 4 , Issue 5 , 2007

Page: [318 - 326] Pages: 9

DOI: 10.2174/157018007780867870

Price: $65


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

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