A convenient synthesis of a selective gelatinase inhibitor as an antimetastatic agent

Compound 1, 2-(4-phenoxyphenylsulfonylmethyl)thiirane, is a potent and selective inhibitor for human gelatinases (J. Am. Chem. Soc. 2000, 122, 6799-6800), enzymes implicated in a number of diseases, including cancer. This compound is showing excellent promise in animal trials in a number of disease models. Large quantities of this compound were necessary for these studies. A convenient four-step synthetic route for compound 1 is described herein. The synthesis is amenable to scale-up to tens of grams and gives an overall yield of 57% for this important compound.     

Pt对Mo基催化剂还原-硫化过程的影响

采用脉冲硫化、连续硫化、程序升温还原、程序升温及程序降温电导及X射线衍射等方法研究了贵金属Pt对MoO3催化剂还原-流化过程的影响及Pt对MOS2配位不饱和活性中心形成的影响．结果表明，Pt担载或在MoO3上可以促进MoO3的还原-硫化，使MoO3的还原-硫化温度大大降低Pt担载在MoSw上可促进MoS2的部分还原形成配位不饱和的钼中心     

A new caffeoyl quinic acid from aster scaber and its inhibitory activity against human immunodeficiency virus-1 (HIV-1) integrase

The phytochemical study of the aerial parts of Aster scaber Thunb. (Asteraceae) yielded a new caffeoyl quinic acid, (-) 3,5-dicaffeoyl-muco-quinic acid (2) and three known compounds, (-) 3,5-dicaffeoyl quinic acid (1), (-) 4,5-dicaffeoyl quinic acid (3), (-) 5-caffeoyl quinic acid (4). The structures were established by high resolution spectroscopic methods. The antiviral effects against HIV-1 integrase of the compounds was evaluated. (-) 3,5-Dicaffeoyl-muco-quinic acid (2) exhibited potent antiviral activity with an IC50 value of 7.0 +/- 1.3 microg/ml.     

Tunable magnetic arrangement of iron oxide nanoparticles in situ synthesized on the solid substrate from diblock copolymer micelles

Hexagonal arrangement of iron oxide nanoparticles was fabricated by utilizing a single-layered film of diblock copolymer micelles. The synthesis was directly performed on the solid substrate by oxygen plasma with preserving the dimensional order of micelles so that separate procedures for synthesis and deposition of nanoparticles were not necessary. Since the oxygen plasma treatment also eliminated polymers, pure patterns of iron oxide nanoparticles were obtained. Moreover, easy control over the size of nanoparticles enabled us to selectively create a ferrimagnetic or a superparamagnetic pattern of iron oxide nanoparticles without altering the fabrication process.