Synthesis and structure-activity relationships of mono- and dialkyl-substituted oxaliplatin derivativesстатья
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Дата последнего поиска статьи во внешних источниках: 18 июля 2013 г.
Авторы:
Habala L. ,
Galanski M. ,
Yasemi A. ,
Nazarov A.A. ,
Von Keyserlingk N.G. ,
Keppler B.K.
Журнал:
European Journal of Medicinal Chemistry
Том:
40
Номер:
11
Год издания:
2005
Издательство:
Elsevier BV
Местоположение издательства:
Netherlands
Первая страница:
1149
Последняя страница:
1155
DOI:
10.1016/j.ejmech.2005.06.003
Аннотация:
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- 1,2-diamine(oxalato)platinum(II) complexes are the most promising candidates to be further evaluated. © 2005 Elsevier SAS. All rights reserved.
Добавил в систему:
Назаров Алексей Анатольевич