Synthesis and antitumor activity of 20-O-linked nitrogen-based camptothecin ester derivatives

Cun-ying Wang; Xian-dao Pan; Hong-yan Liu; Zhao-di Fu; Xian-yong Wei; Li-Xi Yang

doi:10.1016/j.bmc.2004.04.023

Synthesis and antitumor activity of 20-O-linked nitrogen-based camptothecin ester derivatives

Bioorg Med Chem. 2004 Jul 1;12(13):3657-62. doi: 10.1016/j.bmc.2004.04.023.

Authors

Cun-ying Wang¹, Xian-dao Pan, Hong-yan Liu, Zhao-di Fu, Xian-yong Wei, Li-Xi Yang

Affiliation

¹ School of Chemical Engineering and Technology, China University of Mining and Technology, Xuzhou 221008, China.

PMID: 15186850
DOI: 10.1016/j.bmc.2004.04.023

Abstract

A series of nitrogen-based 20S-hydroxyl camptothecin ester derivatives were prepared. 3-Aminopropionate of camptothecin was found more cytotoxic in vitro on several human tumor cell lines than 3-amidopropionate of camptothecin. Ester 16 showed best antitumor activity in vivo and in vitro in all esters we prepared.

MeSH terms

Animals
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / therapeutic use*
Camptothecin / analogs & derivatives
Camptothecin / chemical synthesis*
Camptothecin / chemistry
Camptothecin / therapeutic use*
Cell Line, Tumor
Esters / chemistry*
Female
Humans
Inhibitory Concentration 50
Liver Neoplasms / drug therapy
Liver Neoplasms / pathology
Molecular Structure
Nitrogen / chemistry*
Xenograft Model Antitumor Assays

Substances

Antineoplastic Agents
Esters
Nitrogen
Camptothecin