Application of 17201-43-3In 2021 ,《Novel quinolone-based potent and selective HDAC6 inhibitors: Synthesis, molecular modeling studies and biological investigation》 appeared in European Journal of Medicinal Chemistry. The author of the article were Relitti, Nicola; Saraswati, A. Prasanth; Chemi, Giulia; Brindisi, Margherita; Brogi, Simone; Herp, Daniel; Schmidtkunz, Karin; Saccoccia, Fulvio; Ruberti, Giovina; Ulivieri, Cristina; Vanni, Francesca; Sarno, Federica; Altucci, Lucia; Lamponi, Stefania; Jung, Manfred; Gemma, Sandra; Butini, Stefania; Campiani, Giuseppe. The article conveys some information:
The synthesis of potent and selective quinolone-based histone deacetylase 6 (HDAC6) inhibitors was reported. The quinolone moiety I and II [X= CH, N] was as an innovative bioactive cap-group for HDAC6 inhibition; its synthesis was achieved by applying a multicomponent reaction. The optimization of potency and selectivity of these products was performed by employing computational studies which leded to the discovery of the diethylaminomethyl derivatives II [X= CH, N] as the most promising hit mols. These compounds were investigated in cellular studies evaluated their anticancer effect against colon (HCT-116) and histiocytic lymphoma (U9347) cancer cells, showed good to excellent potency, leaded to tumor cell death by apoptosis induction. The small mols. I, II [X= CH, N] were able to strongly inhibit the cytoplasmic and slightly the nuclear HDAC enzymes, increased the acetylation of tubulin and of the lysine 9 and 14 of histone 3, resp. Compound II [X= CH] was also able to increase Hsp90 acetylation levels in HCT-116 cells, thus further supporting its HDAC6 inhibitory profile. Cytotoxicity and mutagenicity assays of these mols. showed a safe profile; moreover, the HPLC anal. of compound II [X= N] revealed good solubility and stability profile. The results came from multiple reactions, including the reaction of 4-Cyanobenzyl bromide(cas: 17201-43-3Application of 17201-43-3)
4-Cyanobenzyl bromide(cas: 17201-43-3) can reacts with 2H-tetrazole in the presence of KOH to yield 4-[(2H-tetra-zol-2-yl)methyl]benzonitrile. And it may be used in the synthesis of ligands containing a chelating pyrazolyl-pyridine group with a pendant aromatic nitrile.Application of 17201-43-3
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts