Synthesis and cytotoxic activities of 4,5-diarylisoxazoles

Chang-Ming Sun; Lee-Gin Lin; Hsi-Jung Yu; Chih-Yu Cheng; Ya-Chuan Tsai; Chi-Wei Chu; Yi-Hui Din; Yat-Pang Chau; Ming-Jaw Don

doi:10.1016/j.bmcl.2006.11.023

Synthesis and cytotoxic activities of 4,5-diarylisoxazoles

Bioorg Med Chem Lett. 2007 Feb 15;17(4):1078-81. doi: 10.1016/j.bmcl.2006.11.023. Epub 2006 Nov 10.

Authors

Chang-Ming Sun¹, Lee-Gin Lin, Hsi-Jung Yu, Chih-Yu Cheng, Ya-Chuan Tsai, Chi-Wei Chu, Yi-Hui Din, Yat-Pang Chau, Ming-Jaw Don

Affiliation

¹ National Research Institute of Chinese Medicine, No. 155-1, Section 2, Li-Nung Street, Peitou, Taipei 112, Taiwan, ROC.

PMID: 17127061
DOI: 10.1016/j.bmcl.2006.11.023

Abstract

A series of 4,5-diarylisoxazoles related to combretastatin A-4 (CA-4) were synthesized and evaluated for cytotoxicity against three human cancer cell lines. Among them, compound 6e showed better cytotoxic activity than CA-4 in HeLa and HepG2 cell lines assayed with IC(50) value as low as 0.022 and 0.065nM, respectively.

Publication types

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

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology*
Cell Cycle / drug effects
Cell Line, Tumor
Drug Screening Assays, Antitumor
HeLa Cells
Humans
Indicators and Reagents
Isoxazoles / chemical synthesis*
Isoxazoles / pharmacology*
Structure-Activity Relationship

Substances

Antineoplastic Agents
Indicators and Reagents
Isoxazoles