Title of article :
Synthesis, topoisomerase I inhibition and structure–activity relationship study of 2,4,6-trisubstituted pyridine derivatives
Author/Authors :
Long-Xuan Zhao، نويسنده , , Yoon-Soo Moon، نويسنده , , Arjun Basnet، نويسنده , , Eunkyung Kim، نويسنده , , Yurngdong Jahng، نويسنده , , Jae Gyu Park، نويسنده , , Tae Cheon Jeong، نويسنده , , Won-Jea Cho، نويسنده , , Sang-Un Choi، نويسنده , , Chong-Ock Lee، نويسنده , , Sun-Young Lee، نويسنده , , Chong-Soon Lee، نويسنده , , Eung Seok Lee، نويسنده ,
Abstract :
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.
