title: Design and diversity-oriented synthesis of novel 1,4-thiazepan-3-ones fused with bioactive heterocyclic skeletons and evaluation of their antioxidant and cytotoxic activities.
abstract: This study has achieved the design and diversity-oriented synthesis of novel 1,4-thiazepine derivatives embedded with carbazole, pyrazole or isoxazole motif via microwave-assisted multicomponent reactions under solvent-free condition, thus providing a green and facile access to 1,4-thiazepine derivatives with prominent features of high structural diversity, short reaction time, high yields and environmental friendliness. More importantly, these novel compounds have been subjected to the test of in vitro antioxidant and cytotoxic activities, resulting in the finding that these 1,4-thiazepine derivatives not only have significant antioxidant activity, but also exhibit remarkably selective cytotoxicity to carcinoma cell line HCT 116.
authors.affiliation: School of Chemistry and Chemical Engineering, Xuzhou Normal University, Xuzhou 221116, PR China.
authors.forename: Feng
authors.initials: F
authors.lastname: Shi
authors.forename: Xiao-Ning
authors.initials: XN
authors.lastname: Zeng
authors.forename: Xu-Dong
authors.initials: XD
authors.lastname: Cao
authors.forename: Shu
authors.initials: S
authors.lastname: Zhang
authors.forename: Bo
authors.initials: B
authors.lastname: Jiang
authors.forename: Wei-Fa
authors.initials: WF
authors.lastname: Zheng
authors.forename: Shu-Jiang
authors.initials: SJ
authors.lastname: Tu
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology; D000975:Antioxidants / Q000494:pharmacology*; D002227:Carbazoles / Q000737:chemistry; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D045325:HCT116 Cells; D006801:Humans; D008872:Microwaves; D008956:Models, Chemical; D011720:Pyrazoles / Q000737:chemistry; D012997:Solvents; D013696:Temperature; D013841:Thiazepines / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D000975:Antioxidants; D002227:Carbazoles; D011720:Pyrazoles; D012997:Solvents; D013841:Thiazepines; C031280:pyrazole