Inhibition of protein kinase C by dequalinium analogues: Structure–activity studies on head group variations

C Abeywickrama, SA Rotenberg, AD Baker

Index: Abeywickrama, Chandima; Rotenberg, Susan A.; Baker, Arthur David Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 23 p. 7796 - 7803

Full Text: HTML

Citation Number: 10

Abstract

New dequalinium analogues and related heteroaromatic systems were synthesized and evaluated for inhibition of protein kinase Cα. In vitro assays with recombinant human PKCα showed that the number of the aromatic ring head groups as well as their electron-richness, are critical factors that determine potency. The inhibitory strengths of the synthesized compounds are shown to correlate well with Mulliken charges on the head group ring ...

Related Articles:

Allyl amines as ammonia equivalents in the preparation of anilines and heteroarylamines

[Jaime-Figueroa, Saul; Liu, Yanzhou; Muchowski, Joseph M.; Putman, David G. Tetrahedron Letters, 1998 , vol. 39, # 11 p. 1313 - 1316]

Synthesis and in vitro antitubercular activity of a series of quinoline derivatives

[de Souza, Marcus V.N.; Pais, Karla C.; Kaiser, Carlos R.; Peralta, Monica A.; de L. Ferreira, Marcelle; Lourenco, Maria C.S. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 4 p. 1474 - 1480]

Ligandless Copper??Catalyzed Coupling of Heteroaryl Bromides with Gaseous Ammonia

[Fantasia, Serena; Windisch, Johannes; Scalone, Michelangelo Advanced Synthesis and Catalysis, 2013 , vol. 355, # 4 p. 627 - 631]

Synthesis of 3-Sulfonylamino Quinolines from 1-(2-Aminophenyl) Propargyl Alcohols through a Ag (I)-Catalyzed Hydroamination,(2+ 3) Cycloaddition, and an Unusual …

[Aillerie, Alexandre; Pellegrini, Sylvain; Bousquet, Till; Pelinski, Lydie New Journal of Chemistry, 2014 , vol. 38, # 4 p. 1389 - 1391]

4??Quinolylnitrene and 2??quinoxalinylcarbene

[Journal of Physical Organic Chemistry, , vol. 24, # 10 p. 999 - 1008]

More Articles...