Novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives as dual-action hypoglycemic agents that activate GK and PPARc

A series of novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives have been synthesized and evaluated as glucokinase(GK)activators.Ethyl 2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl-amino)thiazole-5-carboxylate was found to be a potent dual-acting hypoglycemic agent activating both GK and PPARg.When given orally to normal mice,the compound demonstrated significant efficacy in decreasing the glucose level after oral glucose loading.

Discovery of novel dual inhibitors of VEGFR and PI3K kinases containing 2-ureidothiazole scaffold

A series of compounds possessing 2-（3-phenyl）ureidothiazol-4-formamide derivatives with a 2-ureidothiazole scaffold were designed and synthesized. Some compounds demonstrated inhibition of cell proliferation against both MDA-MB-231 and Hep G2 cell lines using Sorafenib as the positive control.Compounds 6i showed a good to moderate inhibition on VEGFR-2 and PI3Ka which was proved by further molecular docking study. This study suggests that compound 6i is a potential dual inhibitor of VEGFR-2 and PI3Ka and is applicable for further investigation.

Synthesis and antiproliferative activity of novel 4-substituted-phenoxy-benzamide derivatives

A series of novel 4-substituted-phenoxy-benzamide derivatives bearing an aryl cycloaliphatic amine moiety were synthesized and evaluated for antiproliferative activity against SW620, HT29 and MGC803 cancer cell lines in vitro. The pharmacological data demonstrated that the majority of target compounds exhibited moderate efficacy in HT29 and MGC803 cell lines. Compound 10 c showed promising inhibition of hedgehog（Hh） signaling pathway in an Hh-related assay. In addition, the superposition pattern of 10 c showed a good fit for a pharmacophoric model generated by Hh inhibitors and provided a basis for further structural optimization.

Design,synthesis and biological evaluation of sulfenimine cephalosporin sulfoxides as β-lactamase inhibitors

A series of sulfenimine cephalosporin sulfoxide derivatives （Ta-v） were designed, synthesized and evaluated for their inhibitory activity against TEM-1 and cephalosporinase in cell-free systems. Some of the tested compounds showed enhanced inhibitory activity against class C β-lactamase cephalospor- inase compared with the tazobactam. The most promising compounds 7c and 7n （IC50 ~ 7.6 and 8.6 μmol/L, respectively） were further investigated in combination with cefradine against a variety of clinical isolated fi-lactamase-producing bacterial strains.

Synthesis and biological evaluation of new pyrrolopyrazinone compounds as potential antitumor agents

一系列 pyrrolo [1,2-a ] pyrazinone 混合物(5a9f ) 被综合，并且他们对 SKOV-3 的细胞毒素的活动， A549，在 vitro 的 HeLa 房间被 MTT 方法评估。一些混合物对三根肿瘤房间线显示出潜在的 antitumor 活动。在他们之中，混合物 9c 和 9d 显示出大多数有势力细胞毒素的活动。行动的初步的机制被讨论。

A three-component one-pot synthesis of 2-alkoxy-4-amino-N-arylthiazole-5-carboxamides

A facile and efficient protocol was developed to access 2-alkoxy-4-amino-N-arylthiazole-5-carbox- amides through a three-component one-pot reaction, which involved potassium methyl cyanimido- dithiocarbonate, 2-halo-N-arylacetamides and alcohols. The easy availability and the broad structural diversity of substrates make the reaction useful for the construction of libraries in drug discovery.