69338-35-8Relevant articles and documents
Novel naphthalene-enoates: Design and anticancer activity through regulation cell autophagy
Di Yang, Meng,Shen, Xiao Bao,Hu, Yang Sheng,Chen, Yan Yan,Liu, Xin Hua
, (2019/03/09)
Eleven dihydroxy-2-(1-hydroxy-4-methylpent-3-enyl)naphthalene derivatives as anticancer agents through regulating cell autophagy were designed and synthesized. The anticancer activity results indicated that most compounds manifested obvious un-toxic effec
Direct amide bond formation from carboxylic acids and amines using activated alumina balls as a new, convenient, clean, reusable and low cost heterogeneous catalyst
Ghosh, Sabari,Mukhopadhyay, Chhanda,Bhaumik, Asim,Mondal, John,Mallik, Amit,Sengupta, Sumita
, p. 3220 - 3229,10 (2020/09/16)
For the first time, we have used activated alumina balls (3-5 mm diameter) for amide synthesis from carboxylic acids (unactivated) and amines (unactivated) under neat reaction conditions that produce no toxic by-products and has the advantages of being low-cost, easily available, heterogeneous, reusable and environmentally benign with no troublesome/hazardous disposal of the catalyst.
Dicarboxylic acid azacycle L-prolyl-pyrrolidine amides as prolyl oligopeptidase inhibitors and three-dimensional quantitative structure-activity relationship of the enzyme-inhibitor interactions
Jarho, Elina M.,Wallén, Erik A. A.,Christiaans, Johannes A. M.,Forsberg, Markus M.,Ven?l?inen, Jarkko I.,M?nnist?, Pekka T.,Gynther, Jukka,Poso, Antti
, p. 4772 - 4782 (2007/10/03)
A series of dicarboxylic acid azacycle L-prolyl-pyrrolidine amides was synthesized, and their inhibitory activity against prolyl oligopeptidase (POP) from porcine brain was tested. Three different azacycles were tested at the position beyond P3 and six different dicarboxylic acids at the P3 position. L-Prolyl-pyrrolidine and L-prolyl-2(S)-cyanopyrrolidine were used at the P2-Pl positions. The IC50 values ranged from 0.39 to 19000 nM. The most potent inhibitor was the 3,3-dimethylglutaric acid azepane L-prolyl-2(S)- cyanopyrrolidine amide. Molecular docking (GOLD) was used to analyze binding interactions between different POP inhibitors of this type and the POP enzyme. The data set consisted of the novel inhibitors, inhibitors published previously by our group, and well-known reference compounds. The alignments were further analyzed using comparative molecular similarity indices analysis. The binding of the inhibitors was consistent at the P1-P3 positions. Beyond the P3 position, two different binding modes were found, one that favors lipophilic structures and one that favors nonhydrophobic structures.
