Zaib, Sumera published the artcileEvaluation of indole-picolinamide hybrid molecules as carbonic anhydrase-II inhibitors: Biological and computational studies, HPLC of Formula: 32333-53-2, the publication is Journal of Molecular Structure (2022), 133048, database is CAplus.
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 ± 0.009μM. The inhibition potency was about 22-fold higher than the standard drug acetazolamide (IC50 = 0.9618 ± 0.180μM). 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 ± 3.791μg/mL and 4.128 ± 1.473μg/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.
Journal of Molecular Structure published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3ClINS, HPLC of Formula: 32333-53-2.
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