Ma, Sheng published the artcileDevelopment of Second-Generation Small-Molecule RhoA Inhibitors with Enhanced Water Solubility, Tissue Potency, and Significant in vivo Efficacy, Safety of (E)-3-(3-Nitrophenyl)acrylic acid, the publication is ChemMedChem (2015), 10(1), 193-206, database is CAplus and MEDLINE.
RhoA, a member of the Rho GTPases, is involved in a variety of cellular functions and could be a suitable therapeutic target for the treatment of cardiovascular diseases. However, few small-mol. RhoA inhibitors have been reported. Based on the previously reported lead compounds, 32 new 2-substituted quinoline (or quinoxaline) derivatives were synthesized and tested in biol. assays. Six compounds showed high RhoA inhibitory activities, with IC50 values of 1.17-1.84 ¦ÌM. Among these, I and II demonstrated noticeable vasorelaxation effects against phenylephrine-induced contraction in thoracic aorta artery rings, and compound I had good water solubility and showed significant in vivo efficacy, which was similar to that of 5-(1,4-diazepane-1-sulfonyl)isoquinoline (fasudil) in a subarachnoid hemorrhage-cardiovascular model. To the best of the knowledge, compound I is the first example of a small- mol. RhoA inhibitor with potent in vivo efficacy, which could serve as a good lead for designing cardiovascular agents.
ChemMedChem published new progress about 1772-76-5. 1772-76-5 belongs to catalysis-chemistry, auxiliary class Benzenes, name is (E)-3-(3-Nitrophenyl)acrylic acid, and the molecular formula is C9H7NO4, Safety of (E)-3-(3-Nitrophenyl)acrylic acid.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia