Regioselective synthesis and cytotoxicities of camptothecin derivatives modified at the 7-, 10- and 20-positions

Xian-dao Pan; Rui Han; Piao-yang Sun

doi:10.1016/j.bmcl.2003.08.012

Regioselective synthesis and cytotoxicities of camptothecin derivatives modified at the 7-, 10- and 20-positions

Bioorg Med Chem Lett. 2003 Nov 3;13(21):3739-41. doi: 10.1016/j.bmcl.2003.08.012.

Authors

Xian-dao Pan¹, Rui Han, Piao-yang Sun

Affiliation

¹ Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. xdp@imm.ac.cn

PMID: 14552770
DOI: 10.1016/j.bmcl.2003.08.012

Abstract

A series of 7-acyloxymethylcamptothecin and 20-O-acyl-7-acyloxymethylcamptothecin derivatives were regioselectively prepared on different solvents. 7-Acyloxymethylcamptothecins possess more efficacy than 20-O-acyl-7-acyloxymethylcamptothecins against six human cancer cell lines in vitro.

MeSH terms

Antineoplastic Agents, Phytogenic / chemical synthesis*
Antineoplastic Agents, Phytogenic / pharmacology*
Camptothecin / analogs & derivatives*
Camptothecin / chemical synthesis
Camptothecin / pharmacology*
Cell Line, Tumor
Drug Screening Assays, Antitumor
Humans
Indicators and Reagents
Magnetic Resonance Spectroscopy
Solvents
Structure-Activity Relationship

Substances

Antineoplastic Agents, Phytogenic
Indicators and Reagents
Solvents
Camptothecin