期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 7, 页码 3200-3206出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.03.013
关键词
SN-38; Derivatives; Cytotoxicity; Topo I inhibition
资金
- National Natural Science Foundation of China [30600052]
- Program for New Century Excellent Talents in University [NCET-06-0329]
- Young Science Foundation of Heilongjiang Province [QC08C30]
- State Forestry Administration [2007-12]
A series of 10-position substituted nitrogenous heterocyclic aromatic group derivatives of SN-38 were prepared. Most of these compounds possessed lower cytotoxicities than CPT. Compound 13 revealed potent cytotoxicity similar to CPT, and compounds 17, 18, and 19 showed similar cytotoxic activity to topotecan. All of the pyridine salt derivatives (7-16) revealed comparable or superior topo I inhibitory activity in relation to CPT. Ethyl in the 7-position of these compounds can increase the cytotoxicity and inhibitory activity to topo I compared with corresponding pyridine salts CPT derivatives (7a-13a) and simultaneously maintain good water solubility. This result is consistent with the SAR of CPT. Crown Copyright (C) 2010 Published by Elsevier Masson SAS. All rights reserved.
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