Synthesis, Biochemical Characterization, and in-Silico Investigations of Acyl-3-(Ciprofloxacinyl) Thioureas as Inhibitors of Carbonic Anhydrase-II

Exploring the latest trends in chemistry, structure, coordination, and diverse applications of 1-acyl-3-substituted thioureas: a comprehensive review

“…Anticancer activity of the complexes was comparable to that of Cisplatin. Compound (133) was more potent than other complexes with IC 50 values of 8.6 (HeLa), 8.8 (MCF7) and 9.4 (A549) mM. It was also found that the complexes showed better activity than the acyl thiourea ligands, the reason being their better binding ability (Fig.…”

“…79). 133 In vivo investigation of a new series of acyl thiourea (157a-l) was performed for acetyl hydroxylate synthase (AHAS) enzyme activity inhibition. Almost all compounds showed inhibition activity at a concentration of 100 mg L −1 .…”

Molecular Spectroscopy Evidence of 1,3,5-Tris(4-carboxyphenyl)benzene Binding to DNA: Anticancer Potential along with the Comparative Binding Profile of Intercalation via Modeling Studies

“…A ligand molecule’s spectral alterations may produce a hyperchromic or hypochromic effect in the presence of DNA, with or without a peak shift towards a longer or shorter wavelength. The decrease or increase in peak intensity along with the shift in the red and blue wavelengths suggested that a compound and DNA intercalated through intercalative interaction; the increase in peak intensity suggested that the cationic part of the ligand may have electrostatically bound to the anionic part (PO 4 3− ) of the DNA backbone; and the spectral variation in terms of hypo- or hyperchromic effect with no or minimal shift in peak position (6–8 nm) suggested a weaker molecule [ 49 , 50 , 51 ]. The H3BTB and HS-DNA spectral profiles each displayed a single peak at 328 nm and 260 nm, respectively.…”

Chemistry of heterocycles as carbonic anhydrase inhibitors: A pathway to novel research in medicinal chemistry review

“…Also, these derivatives inhibited hCA IX and XII in K i range of 19.7-353.3 and 8.7-643.7 nM, respectively [45] (Scheme 26). Newly synthesized compounds were screened for their inhibitory activity against hCA II by taking AAZ as a standard drug and it was observed that compound 240g (R = chlorophenyl) showed excellent activity with IC 50 value of 0.97 ± 0.11 µM [46] (Scheme 27). Newly synthesized compounds were evaluated for inhibitory activity against cytosolic hCA I and II as well as transmembrane isoforms hCA IV, IX, and XII by an esterase assay by taking AAZ as standard drug and it was observed that compound 247a (R = phenyl) showed potent activity against hCA IX with K i value of 18.29 nM and compound 247h (R = 2-naphthyl) showed potency against hCA XII with K i value of 9.22 nM.…”