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Browsing by Author Pham, The Hai

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Design, Synthesis and Evaluation of Novel (E)-N'-((1-(4-chlorobenzyl)-1H-indol-3- yl)methylene)-2-(4-oxoquinazolin-3(4H)-yl)acetohydrazides as Antitumor Agents

Authors: Do, Thi Mai Dung; Eun, Jae Park; Duong, Tien Anh; Pham, The Hai; Le, Quang Bao; Advisor: -; Co-Author: - (2022)

Herein, we have designed and synthesized a series of the novel (E)-N'-((1-(4-chlorobenzyl)- 1H-indol-3-yl)methylene)-2-(4-oxoquinazolin-3(4H)-yl)acetohydrazides (5) as potent small molecules activating procaspase- 3. The compounds were designed by the amalgamation of structural features of PAC-1 (the first procaspase-3 activator) and oncrasin-1, one potential anticancer agent

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–activi...