Synthesis, evaluation of in vitro cytotoxic activity, and in silico studies of some 3-methylenamino-4(3H)-quinazolone derivatives

Tuyen Ngoc Truong; Em Canh Pham; Ngoc-Vi Nguyen Tran; Thuan Minh Tieu; M Cao; Tuoi Thi Hong; Khanh N. B. Le

doi:10.1039/d5ra03933a

January 1, 2025RSC AdvancesOpen Access

Synthesis, evaluation of in vitro cytotoxic activity, and in silico studies of some 3-methylenamino-4(3H)-quinazolone derivatives

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Key Points

Compounds 5, 6, and 7 exhibited significant cytotoxic effects against RD and MDA-MB-231 cells, with low toxicity to normal cells.
Cytotoxicity results showed strong binding to EGFR, indicating potential for targeted cancer treatments in future studies.
Twenty novel quinazolone derivatives were synthesized through imine formation, demonstrating promise for cancer applications.
Good ADMET profiles suggest these derivatives may lead to viable therapeutic options, yet further studies are warranted.

Implication

Cytotoxicity against cancer cells was evaluated in vitro, suggesting potential for EGFR-targeting therapies.

Abstract

Twenty 3-methylenamino-4(3 H )-quinazolone derivatives were synthesized via imine formation. Compounds 5, 6, and 7 showed potent cytotoxicity against RD and MDA-MB-231, low toxicity to normal cells, and strong EGFR binding, with good ADMET profiles.

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Cite This Study

Truong et al. (2025) studied this question.

synapsesocial.com/papers/68af540fad7bf08b1eadb2eb https://doi.org/10.1039/d5ra03933a

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Synthesis, evaluation of in vitro cytotoxic activity, and in silico studies of some 3-methylenamino-4(3H)-quinazolone derivatives

Key Points

Implication

Abstract

Discussion

Cite This Study

Synthesis, evaluation of in vitro cytotoxic activity, and in silico studies of some 3-methylenamino-4(3H)-quinazolone derivatives

Key Points

Implication

Abstract

Discussion

Cite This Study

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