ROBINA I.

Cancer cells are highly dependent on Nicotinamide phosphoribosyltransferase (NAMPT) activity for prolifera-tion, therefore NAMPT represents an interesting target for the development of anti-cancer drugs. Several com-pounds, such as FK866 and CHS828, were identified as potent NAMPT inhibitors with strong anti-cancer activity, although none of...

Novel pyrrolidine 3,4-diol derivatives of the type (2R and 2S,3R,4S)-{[((1R)-1-methoxycarbonyl and hydroxylmethyl)-1-arylmethyl)amino]ethyl}-pyrrolidine-3,4-diol have been prepared and evaluated as α-mannosidase inhibitors and assayed for their anticancer activity in vitro. They all exhibit specific but moderate activity as inhibitors towards...

Abstract: Sirtuin 6 (SIRT6) is an NAD+-dependent deacetylase regulating important functions: modulators of its enzymatic activity have been considered as possible therapeutic agents. Besides the deacetylase activity, SIRT6 also has NAD+-dependent deacylase activity, whereby it regulates the secretion of cytokines and proteins. We identified...

A series of new amphiphilic pyrrolidines containing dodecyl and oleylapolar side chains were prepared and evaluated for theirability to inhibit the growth of pancreatic ductal adenocarcinoma cells in vitro. The new compounds are shown to exhibit anticanceractivity at concentrations in the microM range.