2-苯基-苯并异硒唑酮-3及其衍生物的合成和抗肿瘤活性的初步研究

微量元素硒能防治克山病、大骨节病、肿瘤及心血管病等。目前,普遍认为在哺乳动物体内存在着一种重要的含硒酶即谷胱甘肽过氧化物酶(GSH-Px),阻由于其结构的复杂性,限制了对它的研究。而有关硒酶模拟化合物2-苯基-苯并异硒唑酮-3(简称Ebselen)的生物活性已见诸报道,它是具有类似谷胱甘肽过氧化物酶生物活性的小分子有机硒化合物,具有极     

Synthesis,Properties and Crystal Structure of A New 12-Molybdogermanic Salt of Lanthanum Coordinated to N -Methyl-2-Pyrrolidone

A new compound [La(NMP) 4 (H 2 O) 4 ][HGeMo 12 O 40 ]·2NMP·3H 2 O (NMP = N -methyl-2-pyrrolidone), 1 , was synthesized and characterized. The compound crystallizes in the monoclinic space group P 2 1 / c with a = 17.3428(4), b = 18.3258(5), c = 23.0387(7) Å, g = 107.088(1)°, V = 6998.9(3) Å 3 and Z = 4. The structure was characterized crystallographically with final R 1 = 0.0589, wR 2 = 0.1596. The crystal structure contains [GeMo 12 O 40 ] 4 m anions combining with [La(NMP) 4 (H 2 O) 4 ] 3+ cations through hydrogen bonds. The La 3+ ion exhibits eight-coordination with four water molecules and four carbonyl oxygen atoms of the organic ligands. Hydrogen bonds are formed between [GeMo 12 O 40 ] 4 m anions and coordinated water molecules, coordinating to water molecules. The anti-tumor activity of 1 was estimated against Hela and P c -3m cancer cells.     

An efficient protocol for the synthesis of benzoheterocyclic compounds via solid-state melt reaction (SSMR)

An efficient protocol for the synthesis of biologically active benzoheterocyclic compounds such as benzothiazoles, benzimidazoles, benzospirothiazoles, and quinoxaline scaffolds have been accomplished via solid state melt reaction (SSMR) with excellent yields. The new protocol does not require any catalyst, solvent, and workup. Two anti-tumor agents have been prepared to demonstrate the application of this new method.     

Synthesis and in vitro biological evaluation of farnesylthiosalicylic acid derivatives as anti-tumor carcinoma agents

Novel farnesylthiosahcylic acid(FTA) derivatives 5a-m with different substituted 1,3,4-thiadiazoles were synthesized. Compounds 5b,5c,5e and 5f displayed anti-tumor activities superior to FTA in most cancer cells tested.Furthermore,5e induced tumor cell apoptosis,which was accompanied by lower Bcl-2 expression,but with higher Bax and caspase 3 expression activities in cancer cells.