Synthesis of 2,4,6-Tripyridyl Pyridines, and Evaluation of Their Antitumor Cytotoxicity, Topoisomerase I and II Inhibitory Activity, and Structure-activity Relationship

Bulletin of the Korean chemical society

Eung-Seok Lee¹  Hoyoung Choi¹  Young-Shin Kwak¹  Byeong-Seon Jeong¹ 

关键词: Terpyridine;    2;    4;    6-Tripyridyl pyridine;    Topoisomerase inhibition;    Cytotoxicity;    SAR study;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

A series of 2,4,6-tripyridyl pyridines were synthesized, and evaluated for their antitumor cytotoxicity, topoisomerase I and II inhibitory activity. From the eighteen prepared compounds, compounds 10-12 have shown better or similar cytotoxicity against several human cancer cell lines as compared to 2,2`:6`,2``- terpyridine and doxorubicin. Especially, compound 10 exhibited the most potent cytotoxicity better than positive controls. Structure-activity relationship study indicated that 2,2`:6`,2``-terpyridine skeleton has an important role in displaying significant cytotoxicity against several human cancer cell lines.

【 授权许可】

Unknown