Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 40, Issue 11, Pages 1149-1155Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2005.06.003
Keywords
platinum; anticancer complexes; oxaliplatin; cytotoxic activity; structure-activity relationships (SAR)
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In order to improve the pharmacological profile of the anticancer drug oxaliplatin, (trans-R,R-cyclohexane-1,2-diamine)oxalatoplatinum(II), and to explore activity-structure relationships, new mono- and dialkyl substituted oxaliplatin analogues have been synthesized. Following a new synthetic strategy, racemates with a defined stereochemistry at carbon atoms 1, 2, 4, and 5 of the cyclohexane ring could be prepared, which are the bases for reliable structure-activity relationships and the following enantiomer resolution. The cytotoxicity was evaluated in nine tumor cell lines, indicating that bulky substituents have a negative influence on the cytotoxic potency of the oxaliplatin derivatives. With respect to the antiproliferative properties, the 4-methyl-, cis-4,5-dimethyl-, and especially the 4,4-dimethyl-trans-cyclohexane-1,2diamine(oxalato)platinum(II) complexes are the most promising candidates to be further evaluated. (c) 2005 Elsevier SAS. All rights reserved.
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