Synthesis and acrosin inhibitory activity of substituted 4-amino-N-(diaminomethylene) benzenesulfonamide derivatives

A series of new substituted 4-amino-N-(diaminomethylene) benzenesulfonamides were synthesized and their in vitro acrosin inhibitory activities were evaluated. Most of the compounds showed potent acrosin inhibitory activities with compounds 4o and 4p being significantly more potent than the control compound N-alpha-tosyl-l-lysyl-chloromethyl-ketone (TLCK). The compounds provide a new scaffold for the development of acrosin inhibitory agents.     

The evolving biology of small molecules: controlling cell fate and identity

Small molecules have been playing important roles in elucidating basic biology and treatment of a vast number of diseases for nearly a century, making their use in the field of stem cell biology a comparatively recent phenomenon. Nonetheless, the power of biology-oriented chemical design and synthesis, coupled with significant advances in screening technology, has enabled the discovery of a growing number of small molecules that have improved our understanding of stem cell biology and allowed us to manipulate stem cells in unprecedented ways. This review focuses on recent small molecule studies of (i) the key pathways governing stem cell homeostasis, (ii) the pluripotent stem cell niche, (iii) the directed differentiation of stem cells, (iv) the biology of adult stem cells, and (v) somatic cell reprogramming. In a very short period of time, small molecules have defined a perhaps universally attainable naive ground state of pluripotency, and are facilitating the precise, rapid and efficient differentiation of stem cells into somatic cell populations relevant to the clinic. Finally, following the publication of numerous groundbreaking studies at a pace and consistency unusual for a young field, we are closer than ever to completely eliminating the need for genetic modification in reprogramming.     

Substrate-controlled chemoselective synthesis and potent cytotoxic activity of novel 5,6,7-triarylpyrido[2,3-d]pyrimidin-4-one derivatives

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.     

Pharmacophore-based discovery of triaryl-substituted imidazole as new telomeric G-quadruplex ligand

Discovery of potent and selective ligands for telomeric G-quadruplex DNA is a challenging work. Through a combination approach of pharmacophore model construction, model validation, database virtual screening, chemical synthesis and interaction evaluation, we discovered and confirmed triaryl-substituted imidazole TSIZ01 to be a new telomeric G-quadruplex ligand with potent binding and stabilizing activity to G-quadruplex DNA, as well as a 8.7-fold selectivity towards telomeric G-quadruplex DNA over duplex DNA.     

Syntheses and initial evaluation of a series of indolo-fused heterocyclic inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus

Herein, we present initial SAR studies on a series of bridged 2-arylindole-based NS5B inhibitors. The introduction of bridging elements between the indole N1 and the ortho-position of the 2-aryl moiety resulted in conformationally constrained heterocycles that possess multiple additional vectors for further exploration. The binding mode and pharmacokinetic (PK) properties of select examples, including: 13-cyclohexyl-6-oxo-6,7-dihydro-5H-indolo[2,1-d][1,4]benzodiazepine-10-carboxylic acid (7) (IC₅₀ = 0.07 μM, %F = 18), are reported.     

青海省雏蝗属一新种(直翅目,网翅蝗科)

记述采自青海省网翅蝗科雏蝗属1新种,达坂山雏蝗Chorthippus dabanshanensis sp.nov.。模式标本保存于青海师范大学生命与地理科学学院动物标本室。     

中国柱角水虻属二新种(双翅目,水虻科)(英文)

记述我国柱角水虻属2新种,即黄跗柱角水虻Beris flava sp.nov.,舟曲柱角水虻B.zhouquensis sp.nov.。模式标本保存在中国农业大学昆虫博物馆和中国科学院动物研究所。1黄跗柱角水虻,新种Beris flavasp.nov.(图1～3)新种与端褐柱角水虻B.fuscipes Meigen近似,但复眼的毛短而稀疏,生殖背板无背侧突,生殖突长钩状。正模♂,宁夏径源龙潭,1880m,2008-07-05,刘经贤。副模1♂,同正模。2舟曲柱角水虻,新种Beris zhouquensis sp.nov.(图4～6)新种与指突柱角水虻B.digitata Li,Zhanget Yang近似,但跗节全黑色,生殖突基部无突起。正模♂,甘肃舟曲沙滩林场,2400m,1999-07-17,王洪建。副模1♂,同正模,1999-07-16,姚建采。     

三种接种物启动Anammox-EGSB反应器的性能

为了优选接种物和加速Anammox反应器启动,分别以厌氧产甲烷污泥 (Anaerobic methanogenic sludge,AMS)、新鲜厌氧氨氧化污泥 (Fresh Anammox sludge,FAS) 和储藏厌氧氨氧化污泥 (Stored Anammox sludge,SAS) 作为接种物,研究了厌氧氨氧化膨胀颗粒污泥床 (Anammox-EGSB) 反应器 (R1、R2和R3) 的启动性能。结果表明：3种接种物均能成功启动Anammox-EGSB反应器,启动性能的优劣次序为：R2 (接种物为     

采用高效液相色谱技术分析烟草体内的维生素B6化合物

维生素B6 (VB6)是一类化合物的总称.近年来研究发现VB6在植物体内发挥抗逆作用.烟草作为模式植物其体内VB6的存在形态还未见报道.本研究采用高效液相色谱结合荧光检测技术对烟草体内VB6的存在形态进行了分析.结果表明:土壤栽培烟草叶、茎和根中VB6的含量依次为2.9、1.7、3.0 μg/g鲜重;组培烟草叶片的VB...