Novel heterodimers of tetrahydroacridines and tetrahydroquinolinones are disclosed. The heterodimers are capable of acting as both acetylcholinesterase inhibitors and N-methyl-D-aspartate (NMDA) receptor antagonists. The heterodimers may be used to improve cognitive defects via treatment or prevention in both humans and non-humans.
Facile Synthesis of Acridine Derivatives by ZnCl<sub>2</sub>-Promoted Intramolecular Cyclization of <i>o</i>-Arylaminophenyl Schiff Bases
作者:Qing Su、Pei Li、Mina He、Qiaolin Wu、Ling Ye、Ying Mu
DOI:10.1021/ol402732n
日期:2014.1.3
A concise and efficient method for the synthesis of a wide range of acridine derivatives and polycyclic aza-aromatic compounds from a ZnCl2-promoted cyclization reaction of readily available o-arylaminophenyl Schiff base compounds under convenient conditions was developed. Reaction conditions and scope of the new method were examined in detail.
Facile synthesis of acridines via Pd(0)-diphosphine complex-catalyzed tandem coupling/cyclization protocol
作者:Ting-Jun Wang、Wen-Wen Chen、Yi Li、Ming-Hua Xu
DOI:10.1039/c5ob00755k
日期:——
A facile and efficient approach for the synthesis of a variety of acridines via the tandemcoupling/cyclization of substituted 2-bromobenzaldehydes and anilines is described. The reaction can be accomplished with ease in the presence of a catalytic amount of Pd2(dba)3 and diphosphine ligand dppf, providing a broad range of substituted acridines in good to excellent yields (up to 99%). The Lewis acid
[EN] WATER SOLUBLE 4-AZAPODOPHYLLOTOXIN ANALOGS<br/>[FR] ANALOGUES DE 4-AZAPODOPHYLLOTOXINE SOLUBLES DANS L'EAU
申请人:CENTRE NAT RECH SCIENT
公开号:WO2015107119A1
公开(公告)日:2015-07-23
The present invention relates to 4-azapodophyllotoxin analogs of formula (I) in which X, R1, R2, R3, R4 and Ar are as defined in claim 1, preferably a pharmaceutically acceptable salt thereof, optionally in the form of a solvate, a composition comprising said analogs, their use as medicament, in particular for the treatment of cancer, and a process for their preparation.
申请人:CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
公开号:US20160333022A1
公开(公告)日:2016-11-17
The present invention relates to 4-azapodophyllotoxin analogs of formula (I) in which X, R
1
, R
2
, R
3
, R
4
and Ar are as defined in claim
1,
preferably a pharmaceutically acceptable salt thereof, optionally in the form of a solvate, a composition comprising said analogs, their use as medicament, in particular for the treatment of cancer, and a process for their preparation.