Synthesis, topoisomerase I inhibition and structure-activity relationship study of 2,4,6-trisubstituted pyridine derivatives.
For the development of new anticancer agents, phenyl, 2-pyridyl, 2-furyl, 2-thienyl, 2-furylvinyl and 2-thienylvinyl substituted derivatives on 2,4,6-position in pyridine moiety were prepared and evaluated for their topoisomerase I inhibitory activity. Among the thirteen prepared compounds, four compounds exhibited strong topoisomerase I inhibitory activity. A structure-activity relationship study indicated that the 2-thienyl-4-furylpyridine skeleton was important for topoisomerase I inhibitory activity.
Department of Chemistry, Liaoning Normal University, Dalian, Liaoning 116-029, PR China.
Long-Xuan
LX
Zhao
Yoon-Soo
YS
Moon
Arjun
A
Basnet
Eun-kyung
EK
Kim
Yurngdong
Y
Jahng
Jae Gyu
JG
Park
Tae Cheon
TC
Jeong
Won-Jea
WJ
Cho
Sang-Un
SU
Choi
Chong Ock
CO
Lee
Sun-Young
SY
Lee
Chong-Soon
CS
Lee
Eung-Seok
ES
Lee
D000818:Animals; D002417:Cattle; D045744:Cell Line, Tumor; D004264:DNA Topoisomerases, Type I / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors; D014908:Triticum / Q000201:enzymology
D004791:Enzyme Inhibitors; D011725:Pyridines; D059004:Topoisomerase I Inhibitors; D004264:DNA Topoisomerases, Type I