Substrate-controlled chemoselective synthesis and potent cytotoxic activity of novel 5,6,7-triarylpyrido[2,3-d]pyrimidin-4-one derivatives |
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Authors: | Shi Feng Ding Jie Zhang Shu Hao Wen-Juan Cheng Chuang Tu Shujiang |
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Institution: | a College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou 215000, PR China b School of Chemistry and Chemical Engineering, Key Laboratory of Biotechnology for Medicinal Plant, Xuzhou Normal University, Xuzhou, Jiangsu 221116, PR China c Clinical Research Center, the First Affiliated Hospital of Nanjing Medical University, Nanjing 210029, PR China |
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Abstract: | The substrate-controlled chemoselective synthesis of novel 5,6,7-triarylpyrido2,3-d]pyrimidin-4-one derivatives has been successfully achieved via microwave-assisted three-component reactions of 2,6-diaminopyrimidin-4(3H)-one, aromatic aldehydes and 1,2-diphenylethanone. This approach has the prominent features of chemoselectivity, diasteroselectivity, atom economy, short reaction time, high yield as well as operational simplicity. Moreover, these novel compounds were subject to the test of in vitro cytotoxicity to carcinoma SW1116 and SGC7901 cells. Most of the tested compounds showed significant cytotoxicity to SW1116 cells and compound 4b exhibited more potent and efficacious cytotoxicity to SGC7901 cells than doxorubicin hydrochloride as positive control. |
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Keywords: | Pyridopyrimidinone Chemoselective synthesis Multi-component reaction Cytotoxicity |
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