Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 54, Issue -, Pages 281-286Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.05.002
Keywords
Electron-withdrawing group; Homocamptothecin; Camptothecin; Anticancer drugs
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Funding
- National Natural Science Foundation of China [81172936, 21102046]
- Shanghai Science and Technology Mission [10ZR1409600]
- Fundamental Research Funds for the Central Universities
- Laboratory of Organic Functional Molecules
- Sino-French Institute of ECNU
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In order to increase the stability of E-ring of homocamptothecins, the electron-withdrawing group -OH or -OAc was induced to alpha position of ring-E lactone. Ten new homocamptothecin analogs were synthesized. Most compounds showed potent in vitro anticancer activity and potent Topo I inhibition, which was equal or superior to that of CPT, SN-38 and 10-HCPT. The stability studies of this series also displayed significant improvement of the stability. (c) 2012 Elsevier Masson SAS. All rights reserved.
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