Synthesis of potent and selective HDAC6 inhibitors led to unexpected opening of a quinazoline ring was written by Moi, Davide;Citarella, Andrea;Bonanni, Davide;Pinzi, Luca;Passarella, Daniele;Silvani, Alessandra;Giannini, Clelia;Rastelli, Giulio. And the article was included in RSC Advances in 2022.Category: iodides-buliding-blocks This article mentions the following:
Histone deacetylase (HDAC) inhibitors are highly involved in the regulation of many pharmacol. responses, which results in anti-inflammatory and anti-cancer effects. In the present work, chemoinformatic analyses were performed to obtain two potent and selective aminotriazoloquinazoline-based HDAC6 inhibitors. We unexpectedly obtained an aminotriazole from a water-driven ring opening of the triazoloquinazoline scaffold. Both compounds were evaluated as HDAC6 inhibitors, resulting in subnanomolar inhibitory activity and high selectivity with respect to class I HDAC1 and HDAC8. Importantly, the compounds were about 3- and 15-fold more potent compared to the reference compound trichostatin A. Addnl., the predicted binding modes were investigated with docking. Considering that the aminotriazole scaffold has never been embedded into the chem. structure of HDAC6 inhibitors, the present study suggests that both the aminotriazoloquinazoline and aminotriazole classes of compounds could be excellent starting points for further optimization of potential anticancer compounds, introducing such novel groups into a relevant and new area of investigation. In the experiment, the researchers used many compounds, for example, 2-Amino-4-iodobenzoic acid (cas: 20776-54-9Category: iodides-buliding-blocks).
2-Amino-4-iodobenzoic acid (cas: 20776-54-9) belongs to iodide derivatives. Typical reactions of alkyl iodides include nucleophilic substitution, elimination, reduction, and the formation of organometallics. The C–I bond is the weakest of the carbon–halogen bonds. These bond strengths correlate with the electronegativity of the halogen, decreasing in the order F > Cl > Br > I.Category: iodides-buliding-blocks
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com