scholarly journals Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists

Molecules ◽  
2021 ◽  
Vol 26 (20) ◽  
pp. 6297
Author(s):  
Mastaneh Safarnejad Shad ◽  
Sandra Claes ◽  
Eline Goffin ◽  
Tom Van Van Loy ◽  
Dominique Schols ◽  
...  

An expansion of the structure–activity relationship study of CXCR4 antagonists led to the synthesis of a series of isoquinolines, bearing a tetrahydroquinoline or a 3-methylpyridinyl moiety as head group. All compounds were investigated for CXCR4 affinity and antagonism in competition binding and calcium mobilization assays, respectively. In addition, the anti-HIV activity of all analogues was determined. All compounds showed excellent activity, with compound 24c being the most promising one, since it displayed consistently low nanomolar activity in the various assays.

RSC Advances ◽  
2016 ◽  
Vol 6 (97) ◽  
pp. 95177-95188 ◽  
Author(s):  
Tazeem Tazeem ◽  
Xin Han ◽  
Qingjun Zhou ◽  
Jingchen Wei ◽  
Po Tien ◽  
...  

A series of adamantine substituted imidazo[1,2-a]pyridine derivatives were developed through a one-pot multi-component Groebke–Blackburn–Bienaymé reaction, among them several compounds were identified to be the potent inhibitors against HIV-1 cells.


2000 ◽  
Vol 530 (1-2) ◽  
pp. 39-47 ◽  
Author(s):  
C.N Alves ◽  
J.C Pinheiro ◽  
A.J Camargo ◽  
M.M.C Ferreira ◽  
A.B.F da Silva

2012 ◽  
Vol 20 (21) ◽  
pp. 6434-6441 ◽  
Author(s):  
Tsukasa Mizuhara ◽  
Shinya Oishi ◽  
Hiroaki Ohno ◽  
Kazuya Shimura ◽  
Masao Matsuoka ◽  
...  

2008 ◽  
Vol 51 (17) ◽  
pp. 5454-5458 ◽  
Author(s):  
Oriana Tabarrini ◽  
Serena Massari ◽  
Dirk Daelemans ◽  
Miguel Stevens ◽  
Giuseppe Manfroni ◽  
...  

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