title: Green chemoselective synthesis of thiazolo[3,2-a]pyridine derivatives and evaluation of their antioxidant and cytotoxic activities.
abstract: The green chemoselective synthesis of thiazolo[3,2-a]pyridine derivatives was achieved in water via microwave-assisted three-component reactions of malononitrile, aromatic aldehydes and 2-mercaptoacetic acid with molar ratios of 2:1:1.5 and 2:2.2:1, respectively. These compounds were subject to the experiments of antioxidant activity and cytotoxicity to carcinoma HCT-116 cells and mice lymphocytes. Nearly all of the tested compounds possessed potent capacities for scavenging free radicals. In addition, most of these compounds showed cytotoxicity to HCT-116 cells and mice lymphocytes with no selectivity. Of these, only thiazolo[3,2-a]pyridine derivative 5d suggested selective cytotoxicity to tumor cell line HCT-116 cells.
authors.affiliation: School of Chemistry and Chemical Engineering, Key Laboratory of Biotechnology for Medicinal Plant, Xuzhou Normal University, Xuzhou, Jiangsu 221116, PR China.
authors.forename: Feng
authors.initials: F
authors.lastname: Shi
authors.forename: Chunmei
authors.initials: C
authors.lastname: Li
authors.forename: Ming
authors.initials: M
authors.lastname: Xia
authors.forename: Kangjie
authors.initials: K
authors.lastname: Miao
authors.forename: Yanxia
authors.initials: Y
authors.lastname: Zhao
authors.forename: Shujiang
authors.initials: S
authors.lastname: Tu
authors.forename: Weifa
authors.initials: W
authors.lastname: Zheng
authors.forename: Ge
authors.initials: G
authors.lastname: Zhang
authors.forename: Ning
authors.initials: N
authors.lastname: Ma
mesh_terms: D000447:Aldehydes / Q000737:chemistry; D000818:Animals; D016166:Free Radical Scavengers / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D045325:HCT116 Cells; D006801:Humans; D008214:Lymphocytes / Q000187:drug effects; D051379:Mice; D008872:Microwaves; D009570:Nitriles / Q000737:chemistry; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D013864:Thioglycolates / Q000737:chemistry
chemical_list: D000447:Aldehydes; D016166:Free Radical Scavengers; D009570:Nitriles; D011725:Pyridines; D013864:Thioglycolates; C017487:2-mercaptoacetate; C000945:dicyanmethane