Potently inhibiting cancer cell migration with novel 3H-pyrazolo[4,3-f]quinoline boronic acid ROCK inhibitors was written by Dayal, Neetu;Mikek, Clinton G.;Hernandez, Delmis;Naclerio, George A.;Yin Chu, Elizabeth Fei;Carter-Cooper, Brandon A.;Lapidus, Rena G.;Sintim, Herman O.. And the article was included in European Journal of Medicinal Chemistry in 2019.Formula: C8H9BO4 This article mentions the following:
Rho-associated protein kinases (ROCKs) are ubiquitously expressed in most adult tissues, and are involved in modulating the cytoskeleton, protein synthesis and degradation pathways, synaptic function, and autophagy to list a few. A few ROCK inhibitors, such as fasudil and netarsudil, are approved for clin. use. Here we present a new ROCK inhibitor, boronic acid containing HSD1590, which is more potent than netarsudil at binding to or inhibiting ROCK enzymic activities. This compound exhibits single digit nanomolar binding to ROCK (Kds < 2 nM) and sub-nanomolar enzymic inhibition profile (ROCK2 IC50 is 0.5 nM for HSD1590; Netarsudil, an FDA-approved drug, inhibited ROCK2 with IC50 = 11 nM under similar conditions). Whereas netarsudil was cytotoxic to breast cancer cell line, MDA-MB-231 (greater than 80% growth inhibition at concentrations greater than 5 μM), HSD1590 displayed low cytotoxicity to MDA-MB-231. Interestingly, at 1 μM HSD1590 inhibited the migration of MDA-MB-231 whereas netarsudil did not. In the experiment, the researchers used many compounds, for example, 3-Formyl-2-methoxyphenylboronic acid (cas: 480424-49-5Formula: C8H9BO4).
3-Formyl-2-methoxyphenylboronic acid (cas: 480424-49-5) belongs to ethers. Relative to alcohols, ethers are generally less dense, are less soluble in water, and have lower boiling points. They are relatively unreactive, and as a result they are useful as solvents for fats, oils, waxes, perfumes, resins, dyes, gums, and hydrocarbons. Vapours of certain ethers are used as insecticides, miticides, and fumigants for soil. Autoxidation is the spontaneous oxidation of a compound in air. In the presence of oxygen, ethers slowly autoxidize to form hydroperoxides and dialkyl peroxides. If concentrated or heated, these peroxides may explode. To prevent such explosions, ethers should be obtained in small quantities, kept in tightly sealed containers, and used promptly.Formula: C8H9BO4
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem