1,720,986 research outputs found
NON-NATURAL MACROCYCLIC AMIDE HDAC6 INHIBITOR COMPOUNDS AND THEIR USES AS THERAPEUTIC AGENTS
No full textThe present invention relates to novel amide compounds of formula I, and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC6 is responsive, and the pharmaceutical composition containing such compounds
Advances in The Chemical Synthesis of Medium-Sized Cyclitols
No full textDensely hydroxylated, medium-sized carbocycles and their analogues have long been a somewhat neglected molecular progeny for two reasons: (a) the synthesis of such expanded and functionality rich rings is quite a challenging task that remains partially unsolved and (b) the biological significance of these constructs has not yet been thoroughly appreciated. This account mainly discusses recent approaches used to deal with this rare class of carbohydrate mimics with particular emphasis being placed on annulative strategies using ring-closing metathesis, aldol-based ring closure.. intramolecular nitrile oxide and nitrone cycloaddition, and the Claisen rearrangernent. Less documented annulative and non-annulative procedures including free-radical cyclisation, intramolecular coupling, and ring expansion and manipulation are also considered
Towards a Second Generation Approach to Carbocyclic Amino Acid Scaffold and Variants Thereof
No full textEnantioselective Total Synthesis of (1R,3S,4R,5R)-1-Amino-4,5-dihydroxycyclopentane-1,3-dicarboxylic Acid. A Full-Aldol Access to Carbaketose Derivatives
No full textThe enantioselective synthesis of cyclopentanedicarboxylic amino acid 1, a novel rigid and functionalized L-glutamic acid analogue, has been achieved in 15 linear steps from silyloxypyrrole 3, utilizing L-glyceraldehyde 4 as the source of chirality. The key steps in the synthesis are three sequential aldol-based carbon−carbon bond-forming reactions: two crossed vinylogous aldol additions (2 + 3 → 8 and 4 + 5 → 10 + 11) and one intramolecular silylative aldolization (6 → 7). En passant, the short syntheses of (2S)-2-hydroxymethylglutamic acid (16) and its (2R)-enantiomer ent-16, a potent metabotropic glutamate receptor agonist, have been achieved
Vorinostat-Like Molecules as Structural, Stereochemical, and Pharmacological Tools
No full textThe inhibitory activity of an omega-alkoxy analogue of the HDAC inhibitor, Vorinostat (SAHA), against the 11 isoforms of HDAC is described and evaluated with regard to structural biology information retrieved through computational methods. Preliminary absorption and metabolism studies were performed, which positioned this compound as a potential candidate for further preclinical studies and delineated measures for improving its pharmacokinetic profile
Generation and Utility of Novel Enantiopure Surrogates of Glyoxal. Synthesis of Anti-malarial Polysphorin and Related Lignans
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