59472-16-1Relevant academic research and scientific papers
Carbonyl- and sulfur-containing analogs of suberoylanilide hydroxamic acid: Potent inhibition of histone deacetylases
Gu, Wenxin,Nusinzon, Inna,Smith Jr., Ronald D.,Horvath, Curt M.,Silverman, Richard B.
, p. 3320 - 3329 (2007/10/03)
Suberoylanilide hydroxamic acid (SAHA), an inhibitor of histone deacetylase, is used in clinical trials for a variety of advanced cancers. Twelve new analogs of SAHA were synthesized and tested as in vitro inhibitors of isolated histone deacetylases (HDACS) and in vivo inhibitors of interferon regulated transcriptional responses (a marker for HDAC activity). The analogs containing an α-mercaptoketone or an α-thioacetoxyketone were more potent than SAHA in both assays.
Thiazoline derivatives
-
, (2008/06/13)
Object: To provide compounds useful as inhibitors of blood platelet aggregation for intravenous administration. Constitution: A thiazoline derivative represented by the formula: STR1 ?wherein R1 is a hydroxyl group, an alkoxy group, a cycloalkoxy group or a group represented by the formula: R4 NH-- (wherein R4 is a cycloalkyl group), R2 is an alkyl group, a cycloalkyl group or a phenylalkyl group, R3 is a hydrogen atom or an alkyl group, and n is an integer of 2 to 9! or a salt thereof.
A Mechanism for bitter Taste Sensibility in Peptides
Ishibashi, Norio,Kouge, Katsushige,Shinoda,Ichizo,Kanehisa, Hidenori,Okai, Hideo
, p. 819 - 828 (2007/10/02)
To estimate the steric distance between the bitter taste determinant sites in peptides, some cyclic dipeptides, amino acid anilides, amino acid cyclohexylamides, and benzoyl amino acids were synthesized and their tastes were evaluated.The diketopiperazine ring of cyclic dipeptides acted as a bitter taste determinant site due to its hydrophobicity.The steric distance between 2 sites was estimated as 4.1 Angstroem from the molecule models of cyclic dipeptides composed of typical amino acids in the bitter peptides.Due to the hypothesis of two bitter taste determinant sites, which bind with the bitter taste receptor via a "binding unit" and a "stimulating unit," a mechanism for the bitterness in peptides was postulated.
