Synthesis of podophyllotoxin linked β-carboline congeners as potential anticancer agents and DNA topoisomerase II inhibitors

European Journal of Medicinal Chemistry
Manda SathishAhmed Kamal

Abstract

A series of new podophyllotoxin linked β-carboline congeners have been synthesized by coupling various substituted β-carboline acids with 4β-aminopodophyllotoxin. Evaluation of their anticancer activity against a panel of human cancer cell lines such as lung cancer (A549), prostate cancer (DU-145), MDA MB-231 (breast cancer), HT-29 (colon cancer) and HeLa (cervical cancer) suggested that 7i and 7j are the most cytotoxic compounds with IC50values of 1.07 ± 0.07 μM and 1.14 ± 0.16 respectively against DU-145 cell line. Further, detailed biological studies such as cell cycle analysis, topoisomerase II inhibition, Comet assay, DNA binding studies and docking studies have revealed that these congeners are DNA interacting topoisomerase II inhibitors.

Citations

Aug 17, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Xiaofei ChenJie Zhang
Aug 17, 2019·Chemical Record : an Official Publication of the Chemical Society of Japan ... [et Al.]·Nagula ShankaraiahRamya Tokala
Oct 8, 2020·BMC Medical Genomics·Beiwei YuLiqin Zhang
Feb 19, 2021·European Journal of Medicinal Chemistry·Darshana BoraNagula Shankaraiah
Mar 9, 2021·European Journal of Medicinal Chemistry·Shams AaghazAhmed Kamal
Oct 20, 2020·Bioorganic Chemistry·Sangita Dattatray ShindeNagula Shankaraiah
Jun 15, 2021·RSC Medicinal Chemistry·Jay Prakash SoniNagula Shankaraiah
Aug 1, 2021·European Journal of Medicinal Chemistry·Bo Luo, Xinqiang Song
Aug 28, 2021·Frontiers in Cell and Developmental Biology·Hua-Yang FanXin-Hua Liang
Aug 29, 2021·Medicinal Research Reviews·Kritika LaxmikeshavNagula Shankaraiah

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