Evaluation of indole-picolinamide hybrid molecules as carbonic anhydrase-II inhibitors: Biological and computational studies was written by Zaib, Sumera;Khan, Imtiaz;Anbar, Hanan S.;Zaraei, Seyed-Omar;Sbenati, Rawan M.;Maryam, Hafiza Taha;Shah, Hamid Saeed;El-Gamal, Mohammed I.. And the article was included in Journal of Molecular Structure in 2022.Category: chlorides-buliding-blocks This article mentions the following:
The present study reported the successful synthesis and evaluation of a series of indole-picolinamide hybrids I, II [Ar = Ph, 3-CF3C6H4, 3,4-di-ClC6H3], III, IV and V as potent inhibitors of bovine carbonic anhydrase II, a promising therapeutic target for the treatment of neurol. disorders, osteoporosis, glaucoma, cancer and obesity. Various multistep synthetic approaches were utilized to access the desired structures having exclusive sites for chem. modifications and diverse spots for biol. interactions between the ligand and enzyme. Compound I was observed as a potent inhibitor of the bovine CA-II with an IC50 value of 0.0440 卤 0.009渭M. The inhibition potency was about 22-fold higher than the standard drug acetazolamide (IC50 = 0.9618 卤 0.180渭M). Several relevant structure-activity relationships were deduced that enlighten the crucial role of substituents as well as the key pharmacophores involved in the inhibition process. Mol. docking tools reinforced the in vitro assay results. The most active compound I was also investigated for anticancer potential using sulforhodamine B assay and results showed two-fold efficacy against HeLa cells when compared to standard drug cisplatin (IC50 = 8.045 卤 3.791渭g/mL and 4.128 卤 1.473渭g/mL, resp.). These findings were also confirmed by flow cytometry and comet tests. Moreover, fluorescence microscopy with DAPI staining revealed apoptosis as a mechanism of cancer cell death. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Category: chlorides-buliding-blocks).
3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Category: chlorides-buliding-blocks
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics