Design, synthesis, and biological evaluation of resveratrol analogues as aromatase and quinone reductase 2 inhibitors for chemoprevention of cancer
摘要:
A series of new resveratrol analogues were designed and synthesized and their inhibitory activities against aromatase were evaluated. The crystal structure of human aromatase (PDB 3eqm) was used to rationalize the mechanism of action of the aromatase inhibitor 32 (IC50 0.59 mu M) through docking, molecular mechanics energy minimization, and computer graphics molecular modeling, and the information was utilized to design several very potent inhibitors, including compounds 82 (IC50 70 nM) and 84 (IC50 36 nM). The aromatase inhibitory activities of these compounds are much more potent than that for the lead compound resveratrol, which has an IC50 of 80 mu M. In addition to aromatase inhibitory activity, compounds 32 and 44 also displayed potent QR2 inhibitory activity (IC50 1.7 mu M and 0.27 mu M, respectively) and the high-resolution X-ray structures of QR2 in complex with these two compounds provide insight into their mechanism of QR2 inhibition. The aromatase and quinone reductase inhibitors resulting from these studies have potential value in the treatment and prevention of cancer. (C) 2010 Elsevier Ltd. All rights reserved.
Non-linear and potential non-linear optical materials containing molybdenum or tungsten mononitrosyl redox centres. Stilbene derivatives containing ferrocenyl, methoxy or dimethylamino donor groups
作者:Benjamin J. Coe、Thomas A. Hamor、Christopher J. Jones、Jon A. McCleverty、David Bloor、Graham H. Cross、Tony L. Axon
DOI:10.1039/dt9950000673
日期:——
Kurtz powder test for secondharmonicgeneration (SHG). The ferrocenyl derivatives have been found to exhibit SHG on irradiation at 1907 nm, whereas all of the derivatives containing NMe2 or OMe groups are SHG inactive. The crystal structure of [Mo(NO)HB(dmpz)3}ClOC6H4[CHCHC6H4(NMe2-4)]-4}] shows that, although the compound crystallises in a polar space group, the lattice contains pseudocentrosymmetrically
化合物[M(NO)HB(dmpz)3 } X n EC 6 H 4(CH CHC 6 H 3 –R,R')-4} 2- n ](dmpz = 3,5-二甲基吡唑基,n = 1,E = NH,R = [(η 5 -C 5 H ^ 4)的Fe(η 5 -C 5 H ^ 5)] - 4,R'= H; E = O,R = R'= H,E = O或NH,R = 4-OMe,R′= H; R = 4-NMe 2,R′= H; E = NH,R = 2-OMe,R′= 4-OMe; R = 3-OMe ,R'= 4-OMe; R = 2-OMe,R'= 5-OMe; M = Mo,X = Cl或I; M = W,X = Cl;n = 2; E = O,R = R ′= H; E = O或NH,R = 4-OMe或-NMe 2,R′= H;E = NH,R = 2-OMe,R'= 4-OMe; R =
Pigment dispersant with hindered light amine stabilizer and pigment dispersions and coating compositions based thereon
申请人:PPG Industries Ohio, Inc.
公开号:US10557045B2
公开(公告)日:2020-02-11
A pigment dispersion is disclosed comprising (a) at least one pigment and (b) a polymeric dispersant comprising residual units derived from polymerization of a mixture of monomers comprising (b1) at least one ethylenically unsaturated hindered amine light stabilizing monomer and (b2) at least one additional ethylenically unsaturated monomer different from monomer (b1). Coating compositions comprising the same are also disclosed as are substrates coated at least in part with such coatings.
Ethylenically unsaturated amine salts of sulfonic, phosphoric, and carboxylic acids
申请人:Stepan Company
公开号:US20010018461A1
公开(公告)日:2001-08-30
Disclosed are ethylenically unsaturated amine salts of sulfonic, phosphoric and carboxylic acids. The salts are surface active agents which are useful in a variety of applications as primary and/or secondary surfactants. The salts are especially useful as surfactants in emulsion polymerization reactions.
Antimicrobial polymer latexes derived from unsaturated quaternary ammonium compounds and antimicrobial coatings, sealant, adhesives and elastomers produced from such latexes
申请人:Stepan Company
公开号:US20020040092A1
公开(公告)日:2002-04-04
Disclosed are antibacterial CASE materials comprising a latex comprising polymer particles and a surfactant component. Also disclosed are components and methods for forming such materials.
所公开的抗菌 CASE 材料由包含聚合物颗粒和表面活性剂成分的胶乳组成。还公开了形成这种材料的成分和方法。
Emulsion polymerization process utilizing ethylenically unsaturated amine salts of sulfonic, phosphoric and carboxylic acids
申请人:STEPAN COMPANY, A corporation of the State of Delaware
公开号:US20020161108A1
公开(公告)日:2002-10-31
Disclosed is an improved method of making polymers. The method utilizes at least one ethylenically unsaturated monomer and at least one polymerizable surface active agent. The polymerizable surface active agent is capable of co-polymerization with traditional monomers and/or polymerization with itself (i.e. homopolymerization) and is preferably substantially completely consumed during the course of the polymerization. Polymers produced by the method of the present invention are well suited for use in coatings, adhesives, sealants, elastomers and the like, as they form stable films, possess excellent adhesion properties and have improved hydrolytic stability characteristics. The present invention also encompasses homopolymeric surface active agents and their use in polymerization reactions.