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Synthesis and biological activity, and molecular modelling studies of potent cytotoxic podophyllotoxin-naphthoquinone

Ha Thanh Nguyen^1,2, Quynh Giang Nguyen Thi^1,2, Thu Ha Nguyen Thi^1,2

¹Graduate University of Science and Technology, Vietnam Academy of Science and Technology (VAST) 18 Hoang Quoc Viet Cau Giay Hanoi Vietnam ngvtuyen@hotmail.com ngvtuyen@ich.vast.vn.

|August 31, 2022

Abstract:

A new approach for the synthesis of podophyllotoxin-naphthoquinone compounds using microwave-assisted three-component reactions is reported in this study. Novel podophyllotoxin-naphthoquinone derivatives with modification on ring E were synthesized. All the synthetic compounds were assessed in terms of their cytotoxicity profile against four cancer cell lines (KB, HepG2, A549, and MCF7), and noncancerous Hek-293 cell lines. Notably, treatment of SK-LU-1 cells with compounds 5a and 5b resulted in G2/M phase arrest of the cell cycle, caspase-3/7 activation, and apoptosis. Additionally, molecular docking studies were performed and showed important interaction of two compounds against residues in the colchicine-binding-site of tubulin as well. Taken together, compounds 5a and 5b were identified as potent anticancer agents.

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