Browsing by Subject Acetohydrazides

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  • Authors: Do, Thi Mai Dung; Eun, Jae Park; Duong, Tien Anh;  Advisor: -;  Co-Author: - (2022)

    A biological evaluation revealed that all thirteen compounds designed and synthesized showed strong cytotoxicity against three human cancer cell lines (SW620, colon cancer; PC-3, prostate cancer; NCI-H23, lung cancer) with eight compounds (5a, 5c-i, 5k), which were clearly more potent than both PAC-1 and oncrasin-1. In this series, four compounds, including 5c, 5e, 5f, and 5h, were the most potent members with approximately 4- to 5-fold stronger than the reference compounds PAC-1 and oncrasin-1 in terms of IC50. In comparison to 5-FU, these compounds were even 18- to 29-fold more potent in terms of cytotoxicity in three human cell lines tested. In the caspase activation assay, the cas...
  • 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–activi...