6386-41-0Relevant articles and documents
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.
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