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SYNTHESIS AND EVALUATION OF NOVEL CHEMICAL ENTITIES AS ANTI-BREAST CANCER AGENTS

By: Contributor(s): Publication details: Mumbai Indian Drug Manufacture's Association - IDMA 2019Edition: Vol.56(12), DecDescription: 28-31pSubject(s): Online resources: In: Indian drugsSummary: A series of dihydropyrimidone derivatives was synthesized by an efficient, simple and solvent less green method by using Beginelli reaction. Various aromatic aldehydes, urea and ethyl acetoacetate were refluxed for a few hours and the reaction monitored by periodic TLC (hexane: ethyl acetate 6:4 v/v) and products are purified by recrystallization, with characterization by FTIR, 1H NMR. All the purified compounds were subjected to evaluatation by in vitro human breast cancer cell line MDA-MB-231 and MCF-7. Compound I-k was found to be moderately active against MCF-7 with GI 50 value of -4.38.
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A series of dihydropyrimidone derivatives was synthesized by an efficient, simple and solvent less green method by using Beginelli reaction. Various aromatic aldehydes, urea and ethyl acetoacetate were refluxed for a few hours and the reaction monitored by periodic TLC (hexane: ethyl acetate 6:4 v/v) and products are purified by recrystallization, with characterization by FTIR, 1H NMR. All the purified compounds were subjected to evaluatation by in vitro human breast cancer cell line MDA-MB-231 and MCF-7. Compound I-k was found to be moderately active against MCF-7 with GI 50 value of -4.38.

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