Simple exploration of 27828-71-3

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In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Discovery of heterocycle-containing α-naphthoflavone derivatives as water-soluble, highly potent and selective CYP1B1 inhibitors, published in 2021-01-01, which mentions a compound: 27828-71-3, mainly applied to trimethoxy alpha naphthoflavone docking SAR solubility CYP1B1 inhibitor; CYP1 enzymes; CYP1B1 inhibitors; SARs; α-Naphthoflavone derivatives, Related Products of 27828-71-3.

A set of forty-six 6,7,10-trimethoxy-α-naphthoflavone derivatives I [R = 2-furyl, 2-chloro-4-pyridyl, 5-bromo-2-pyridyl, etc.] was synthesized and screened against CYP1 enzymes, leading to the identification of fluorine-containing compound I [R = 5-bromo-2-pyridyl] as the most potent and selective CYP1B1 inhibitor (IC50 value of 0.07 nM), being 84-fold more potent than that of the template mol. ANF. Alternatively, the amino-substituted derivative I [R = 4-amino-3-pyridyl] not only possessed a potent inhibitory effect on CYP1B1 (IC50 value of 0.98 nM), but also had a substantially increased water solubility as compared with the lead ANF. The current study expanded the structural diversity of CYP1B1 inhibitors and compound I [R = 4-amino-3-pyridyl] could be considered as a promising starting point with great potential for further studies.

I hope my short article helps more people learn about this compound(5-Hydroxynicotinic acid)Related Products of 27828-71-3. Apart from the compound(27828-71-3), you can read my other articles to know other related compounds.

Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method