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    • Design, synthesis, and evaluation of novel (E)‐N'‐(3‐allyl‐2‐hydroxy)benzylidene‐2‐(4‐oxoquinazolin‐3(4H)‐yl)acetohydrazides as antitumor agents
    Authors: Do T. M. Dung; Eun J. Park; Duong T. Anh; Pham, The Hai; Le D. Huy; Hye W. Jun; Joo-Hee Kwon; A. Young Ji; Jong S. Kang; Truong T. Tung; Phan T. P. Dung; Sang-Bae Han; Nguyen-Hai Nam;  Advisor: -;  Co-Author: - (2021)

    In our continuing search for novel small‐molecule anticancer agents, we designedand synthesized a series of novel (E)‐N'‐(3‐allyl‐2‐hydroxy)benzylidene‐2‐(4‐oxoquinazolin‐3(4H)‐yl)acetohydrazides (5), focusing on the modification of sub-stitution in the quinazolin‐4(3H)‐one moiety. The biological evaluation showed thatall 13 designed and synthesized compounds displayed significant cytotoxicity againstthree human cancer cell lines (SW620, colon cancer; PC‐3, prostate cancer; NCI‐H23, lung cancer). The most potent compound5ldisplayed cytotoxicity up to 213‐fold more potent than 5‐fluorouracil and 87‐fold more potent than PAC‐1, the firstprocaspase‐activating compound. Structure–activity relationship analysis revealedthat substitution of either electron‐withdrawing or electron‐releas...