Synthesis and antitumor activity of simplified ecteinascidin-saframycin analogs

Zhan-Zhu Liu; Ye Wang; Ye-Feng Tang; Shi-Zhi Chen; Xiao-Guang Chen; Hong-Yan Li

doi:10.1016/j.bmcl.2005.11.069

Synthesis and antitumor activity of simplified ecteinascidin-saframycin analogs

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1282-5. doi: 10.1016/j.bmcl.2005.11.069. Epub 2005 Dec 9.

Authors

Zhan-Zhu Liu¹, Ye Wang, Ye-Feng Tang, Shi-Zhi Chen, Xiao-Guang Chen, Hong-Yan Li

Affiliation

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

PMID: 16338237
DOI: 10.1016/j.bmcl.2005.11.069

Abstract

Two series of simplified analogs of the ecteinascidin-saframycin type alkaloids were prepared from l-DOPA. Their in vitro antitumor activity was tested against three human cancer cell lines (HCT-8 colon carcinoma, Bel-7402 liver carcinoma, and BGC-823 gastric carcinoma). Among these compounds, the ester analogs have stronger activities than those of amide analogs in general. Among them, 1-naphthalene carboxylate ester analog 31 has the strongest activity against BGC-823 cells.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Heterocyclic Compounds, 4 or More Rings / chemical synthesis
Heterocyclic Compounds, 4 or More Rings / chemistry*
Heterocyclic Compounds, 4 or More Rings / pharmacology*
Humans
Isoquinolines / chemical synthesis
Isoquinolines / chemistry*
Isoquinolines / pharmacology*
Molecular Structure
Structure-Activity Relationship

Substances

Antineoplastic Agents
Heterocyclic Compounds, 4 or More Rings
Isoquinolines