2-Thienyl-4-furyl-6-aryl pyridine derivatives: synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study

Bioorganic & Medicinal Chemistry
Pritam ThapaEung-Seok Lee

Abstract

Designed and synthesized 60 2-thienyl-4-furyl-6-aryl pyridine derivatives were evaluated for their topoisomerase I and II inhibitory activities at 20 microM and 100 microM and cytotoxicity against several human cancer cell lines. Compounds 8, 9, 11-29 showed significant topoisomerase II inhibitory activity and compounds 10 and 11 showed significant topoisomerase I inhibitory activity. Most of the compounds (7-21) possessing 2-(5-chlorothiophen-2-yl)-4-(furan-3-yl) moiety showed higher or similar cytotoxicity against HCT15 cell line as compared to standards. Most of the selected compounds displayed moderate cytotoxicity against MCF-7, HeLa, DU145, and K562 cell lines. Structure-activity relationship study revealed that 2-(5-chlorothiophen-2-yl)-4-(furan-3-yl) moiety has an important role in displaying biological activities.

References

Feb 13, 2007·Biochimie·Patrick ForterreMarie-Claude Serre

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Citations

Jan 1, 2012·Journal of Chemical Biology·Muthu K KathiravanMadhuri A Nagras
Feb 26, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Hamada Mohamed Ibrahim, Haider Behbehani
Mar 3, 2012·Journal of Enzyme Inhibition and Medicinal Chemistry·Muthu K KathiravanKishor S Jain
Dec 7, 2011·Journal of Enzyme Inhibition and Medicinal Chemistry·Selçuk AyvazAliye Altuntas
Dec 2, 2014·European Journal of Medicinal Chemistry·Radha KarkiYoungjoo Kwon
May 1, 2015·Organic & Biomolecular Chemistry·Rajni KhajuriaParthasarathi Das
Feb 24, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ahmed MalkiHayam Ashour
Apr 20, 2018·ACS Medicinal Chemistry Letters·Pablo GarnicaCarmen Sanmartín
Oct 9, 2019·Journal of Medicinal Chemistry·Žiga SkokJanez Ilaš

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