3164-07-6

Abstract A simple and efficient one-pot synthesis of 5-(benzoxazol-2'-yl)bicyclo[2.2.2]octen-2-one derivatives from readily accessible starting materials has been demonstrated. The current protocol involves diacetoxyiodobenzene mediated domino oxidative c

The present invention relates to compounds represented by the following Formula (I). With reference to Formula (I), at least one of E1 and E2 independently is, or is independently substituted with, at least one reactive group, such as a (meth)acryloyl group. The compounds of the present invention can be used alone and/or in combination with polymers prepared from such compounds, such as to form or as one or more components of an alignment layer.

A series of benzothiazole and benzoxazole linked pyrrolobenzodiazepine conjugates attached through different alkane or alkylamide spacers was prepared. Their anticancer activity, DNA thermal denaturation studies, restriction endonuclease digestion assay and flow cytometric analysis in human melanoma cell line (A375) were investigated. One of the compounds of the series 17d showed significant anticancer activity with promising DNA-binding ability and apoptosis caused G0/G1 phase arrest at sub-micromolar concentrations. To ascertain the binding mode and understand the structural requirement of DNA binding interaction, molecular docking studies using gold program and more rigorous 2 ns molecular dynamic simulations using Molecular Mechanics-Poisson-Boltzman Surface Area (MM-PBSA) approach including the explicit solvent were carried out. Further, the compound 17d was evaluated for in vivo efficacy studies in human colon cancer HT29 xenograft mice.

A series of potent and selective mGluR5 antagonists were synthesized and evaluated in vitro and in vivo. It was found that a pyridyl functionality is a potential replacement for acetonitrile in the lead structure, with 2-pyridyl being most favored. Additi