ArticleJournal of enzyme inhibition and medicinal chemistry2019
(E)-N'-Arylidene-2-(4-oxoquinazolin-4(3H)-yl) acetohydrazides: Synthesis and evaluation of antitumor cytotoxicity and caspase activation activity.
Article in Journal of enzyme inhibition and medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 24 citations in OpenAlex.
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- Synthesis, cytotoxicity, apoptosis-inducing activity and molecular docking studies of novel isatin-podophyllotoxin hybrids.RSC advances · 2025Article
- Design and biological evaluation of 3-substituted quinazoline-2,4(1Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Polyoxometalate-based nanocomposites for antitumor and antibacterial applications.Nanoscale advances · 2022Review
- Synthesis and biological activity, and molecular modelling studies of potent cytotoxic podophyllotoxin-naphthoquinone compounds.RSC advances · 2022Article
- Design, synthesis and evaluation of novel 2-oxoindoline-based acetohydrazides as antitumor agents.Scientific reports · 2022Article
- Novel 4-Oxoquinazoline-BasedACS omega · 2021Article
- Design, synthesis, and evaluation of novelJournal of enzyme inhibition and medicinal chemistry · 2020Article
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Authors and funding
13 authors at 4 institutions in 2 countries.
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Abstract
In our search for novel small molecules activating procaspase-3, we have designed and synthesised a series of novel acetohydrazides incorporating quinazolin-4(3H)-ones (5, 6, 7). Biological evaluation revealed eight compounds with significant cytotoxicity against three human cancer cell lines (SW620, colon cancer; PC-3, prostate cancer; NCI-H23, lung cancer). The most potent compound 5t displayed cytotoxicity up to 5-fold more potent than 5-FU. Analysis of structure-activity relationships showed that the introduction of different substituents at C-6 position on the quinazolin-4(3H)-4-one moiety, such as 6-chloro or 6-methoxy potentially increased the cytotoxicity of the compounds. In term of caspase activation activity, several compounds were found to exhibit potent effects, (e.g. compounds 7 b, 5n, and 5l). Especially, compound 7 b activated caspases activity by almost 200% in comparison to that of PAC-1. Further docking simulation also revealed that this compound potentially is a potent allosteric inhibitor of procaspase-3.
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