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ID: ALA1147612

Journal: Bioorg Med Chem Lett

Title: Synthesis, topoisomerase I inhibition and structure-activity relationship study of 2,4,6-trisubstituted pyridine derivatives.

Authors: Zhao LX, Moon YS, Basnet A, Kim EK, Jahng Y, Park JG, Jeong TC, Cho WJ, Choi SU, Lee CO, Lee SY, Lee CS, Lee ES.

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.

CiteXplore: 14980693

DOI: 10.1016/j.bmcl.2003.11.084