Rigid Analogues of Antimitotic Indolobenzazepinones: New Insights into Tubulin Binding via Molecular Modeling
摘要:
Two rigid analogues of 5-ethylindolobenzazepinone 4, a potent c-ytotoxic agent and inhibitor of tubulin polymerization, were prepared. The first was the indane derivative 5, in which the ethyl group is attached to the benzo moiety. The second was the pyrrolidine analogue 6, in which the ethyl chain was bound to the lactam nitrogen. While both compounds were considerably less active inhibitors of KB cell growth as compared to 4, inhibition of tubulin polymerization was only moderately reduced. Tubulin docking studies indicated that the aR and aS atropoisomers of 5 and 6 occupy different binding pockets at the colchicine binding site. Conversely, both aS-5 and aS-6 occupy the same binding pocket as aSS-4 but do not benefit from the favorable hydrophobic interactions provided by the CS alkyl group of 4, thus possibly explaining their lower activities.
Microwave-accelerated reductive amination between ketones and ammonium acetate
摘要:
A new procedure for reductive amination between ketones and ammonium acetate has been developed to access a variety of primary amines. This protocol takes advantage of microwave heating to significantly accelerate the reaction and offers a convenient and effective method to access some interesting amines. This new procedure compares favorably to previously reported approaches in terms of practicality, efficiency, and functional group compatibility. (C) 2010 Elsevier Ltd. All rights reserved.
[EN] INDANE AND INDOLINE DERIVATIVES AND THE USE THEREOF AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS<br/>[FR] DÉRIVÉS D'INDANE ET D'INDOLINE ET LEUR UTILISATION EN TANT QU'ACTIVATEURS DE LA GUANYLATE CYCLASE SOLUBLE
申请人:NOVARTIS AG
公开号:WO2016001875A1
公开(公告)日:2016-01-07
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
SUBSTITUTED FLUOROETHYL UREAS AS ALPHA 2 ADRENERGIC AGENTS
申请人:Chow Ken
公开号:US20080255239A1
公开(公告)日:2008-10-16
Therapeutic compounds, and methods, compositions, and medicaments related thereto are disclosed herein.
本文揭示了治疗化合物、方法、组合物和相关药物。
METHODS FOR MAKING QUINOLINYLDIAMINES
申请人:ExxonMobil Chemical Patents Inc.
公开号:US20200071344A1
公开(公告)日:2020-03-05
The present disclosure provides methods for making quinolinyldiamine products from quinolinyl starting materials. In addition, the quinolinyldiamines can be used as ligands or ligand precursors for catalysts, e.g. for use in olefin polymerization.
Disclosed herein is compound having a formula
as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
本文披露了具有如本文所述的化学式的化合物。还披露了与之相关的治疗方法、组成和药物。
[EN] HETEROCYCLIC AMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS D'AMIDE HÉTÉROCYCLIQUE COMME ANTAGONISTES DU RÉCEPTEUR P2X7
申请人:ACTELION PHARMACEUTICALS LTD
公开号:WO2013108227A1
公开(公告)日:2013-07-25
The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, X and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.