6386-41-0Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of bifunctional thyrointegrin inhibitors: New anti-angiogenesis analogs
Bridoux, Alexandre,Khan, Riaz A.,Chen, Celei,Cheve, Gwenael,Cui, Huadong,Dyskin, Evgeny,Yasri, Aziz,Mousa, Shaker A.
, p. 871 - 882 (2011)
Context: Inhibition of pathological angiogenesis. Objective: Obtaining new transactivator, bifunctional, thyroid antagonist, non-toxic anti-angiogenic compounds. Materials and methods: In silico drug design, synthesis in bulk and biological evaluation in chick chorioallantoic membrane (CAM) model. Results: Significant inhibition (range 6573%) at 0.252.0 g/ml doses. Discussion and conclusion: The synthesis of compounds (9), (10), and (11) incorporating long-chain moieties guanidine, urea, methyl amine and, propyl amine substitutions, respectively, into the core molecular framework of tetrac (tetraiodothyroacetic acid) were undertaken. The evaluation of the anti-angiogenic bioactivity of these compounds in the CAM model revealed no loss of activity in comparison with tetrac and XT199, which showed nearly 86% inhibition at dose levels of 1 and 0.5 g/ml, respectively, and validated the concept.
COMPOSITIONS OF DUAL THYROINTEGRIN ANTAGONISTS AND USE IN VASCULAR-ASSOCIATED DISORDERS
-
Page/Page column 11-12, (2011/05/08)
A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and alphavbeta3 integrin antagonist in the same molecule
Inhibitors of lipoprotein(a) assembly
Sexton, Karen E.,Lee, Helen T.,Massa, Mark,Padia, Janak,Patt, William C.,Liao, Peggy,Pontrello, Jason K.,Roth, Bruce D.,Spahr, Mark A.,Ramharack, Randy
, p. 4827 - 4845 (2007/10/03)
Compounds of the general structure A and B were investigated for their activity as lipoprotein(a), [Lp(a)], assembly (coupling) inhibitors. SAR around the amino acid derivatives (structure A) gave compound 14-6 as a potent coupling inhibitor. Oral dosing
Polyalkylene glycol esters of hindered phenols substituted alkanoic acid
-
, (2008/06/13)
Compounds of the formula: EQU1 WHEREIN X is oxygen or sulfur, a is an integer from 2 to 6, b is an integer from 3 to 40, and R is SPC1 Wherein R1 is an alkyl group of 1 to 8 carbon atoms, R2 is hydrogen or an alkyl group of 1 to 8 carbon atoms, and X is an integer from 0 to 6 Are useful as antioxidants for organic materials normally subject to oxidative deterioration, such as polyacetals, polypropylene, and nylon, in amounts of from about 0.005 to about 5% by weight of the composition.
