title: Substrate-controlled chemoselective synthesis and potent cytotoxic activity of novel 5,6,7-triarylpyrido[2,3-d]pyrimidin-4-one derivatives.
abstract: The substrate-controlled chemoselective synthesis of novel 5,6,7-triarylpyrido[2,3-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.
authors.affiliation: College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou, PR China.
authors.forename: Feng
authors.initials: F
authors.lastname: Shi
authors.forename: Jie
authors.initials: J
authors.lastname: Ding
authors.forename: Shu
authors.initials: S
authors.lastname: Zhang
authors.forename: Wen-Juan
authors.initials: WJ
authors.lastname: Hao
authors.forename: Chuang
authors.initials: C
authors.lastname: Cheng
authors.forename: Shujiang
authors.initials: S
authors.lastname: Tu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D000970:Antineoplastic Agents; D011744:Pyrimidinones