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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 34, Number 10
BKCSDE 34(10)
October 20, 2013 

2,4-Diaryl Benzofuro[3,2-b]pyridine Derivatives: Design, Synthesis, and Evaluation of Topoisomerase Inhibitory Activity and Cytotoxicity
Pritam Thapa, Yurngdong Jahng, Pil-Hoon Park, Jun-Goo Jee, Youngjoo Kwon*, Eung-Seok Lee*
2,4-Diaryl benzofuro[3,2-b]pyridine, Topoisomerase I and II inhibition, Cytotoxicity
Designed and synthesized twenty-four 2,4-diaryl benzofuro[3,2-b]pyridine derivatives were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Various aryl groups such as phenyl, 2- or 3- furyl, 2- or 3-thienyl, and 2-pyridyl were substituted at 2- or 4- position of central pyridine. Compounds 8, 12, 13, and 14, with 2-furyl either at 2- or 4- position of central pyridine showed the significant topoisomerase II inhibitory activity at 100 μM.
3073 - 3082
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