Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2':6',2"-, 2,2':6',3"- and 2,2':6',4"-terpyridine derivatives.
For the development of new anticancer agents, 2,2':6',2"-, 2,2':6',3"- and 2,2':6',4"-terpyridine derivatives were designed and evaluated for their topoisomerase I inhibitory activity and antitumor cytotoxicity. Structure-activity relationship studies indicated that 2,2':6',2"-terpyridine derivatives were highly cytotoxic toward several human tumor cell lines, whereas 2,2':6',3"- and 2,2':6',4"-terpyridine derivatives were potent topoisomerase I inhibitors.
Zhao
L X
LX
College of Pharmacy, Yeungnam University, Kyongsan 712-749, South Korea.
Kim
T S
TS
Ahn
S H
SH
Kim
T H
TH
Kim
E K
EK
Cho
W J
WJ
Choi
H
H
Lee
C S
CS
Kim
J A
JA
Jeong
T C
TC
Chang
C J
CJ
Lee
E S
ES
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D019073:HT29 Cells; D006801:Humans; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D059004:Topoisomerase I Inhibitors; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D011725:Pyridines; D059004:Topoisomerase I Inhibitors; C013278:2,2',2''-terpyridine