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Author
- Do T. M. Dung (2)
- Duong T. Anh (2)
- Eun J. Park (2)
- Jong S. Kang (2)
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Subject
- Acetohydrazides (1)
- caspase activation (1)
Date issued
- 2021 (2)
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Two series of novel 4-oxoquinazoline-based N-hydroxypropenamides (9a–m and 10a–m) were designed, synthesized, and evaluated for their inhibitory and cytotoxicity activities against histone deacetylase (HDAC). The compounds showed good to potent HDAC inhib |
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... |