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Design, synthesis, and antitumor evaluation of novel naphthalimide derivatives

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In order to research the structure–activity relationships of novel naphthalimide derivatives bearing disulfide bond toward antitumor activity, we prepared a series of those and their in vitro antiproliferative activities were… Click to show full abstract

In order to research the structure–activity relationships of novel naphthalimide derivatives bearing disulfide bond toward antitumor activity, we prepared a series of those and their in vitro antiproliferative activities were screened against human cancer cell lines A549, Hela, SMMC-7721, and normal cell lines L929 by CCK-8 assay. After testing, most of synthesized compounds 5a-i , 6a-i showed better antitumor activity than the positive control 5-fluorouracil. Compounds 5b , 5f , and 5i showed excellent antitumor activity against Hela cells with IC 50 values of 3.64, 3.67, and 3.57 µM, respectively. Compounds 5a , 5b , and 5i exhibited good biological activity to A549 cells with IC 50 values of 5.25, 6.20, and 5.50 respectively. Compared with 5-fluorouracil, all of synthesied compounds showed low cytotoxic effects on normal human cell line L929.

Keywords: naphthalimide derivatives; antitumor activity; compounds showed; novel naphthalimide; antitumor; activity

Journal Title: Medicinal Chemistry Research
Year Published: 2019

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