Design, synthesis, and antitumor evaluation of 2,4,6-triaryl pyridines containing chlorophenyl and phenolic moiety

作者：Thapa Pritam; Karki Radha; Yun Minho; Kadayat Tara Man; Lee Eunyoung; Kwon Han Byeol; Na Younghwa; Cho Won Jea; Kim Nam Doo; Jeong Byeong Seon; Kwon Youngjoo; Lee Eung Seok^*

来源：European Journal of Medicinal Chemistry, 2012, 52: 123-136.

DOI：10.1016/j.ejmech.2012.03.010

• 2,4,6-Triaryl pyridine
• Antitumor
• Terpyridine
• Topoisomerase I and II inhibition
• Cytotoxicity

We have designed and synthesized a series of 2,4,6-triaryl pyridine derivatives containing chlorophenyl and phenolic moeity at 2- and 4- position of the central pyridine, respectively, resulting in a total of 42 compounds. They were evaluated for topoisomerase I and 11 inhibitory activities as well as cytotoxicities against several human cancer cell lines. Most compounds showed better topoisomerase II inhibitory activity compared to topoisomerase 1 inhibitory activity. Compounds 19, 20, 26-28, and 47-50 especially showed stronger topo II inhibitory activity than etoposide.

• 出版日期2012-6