Synthesis and in vitro antitumour activity of tiazofurin analogues with nitrogen functionalities at the C-2′ position

Thiazoles in glycosylation reactions: Novel synthesis of thiazole thioglycosides

“…The IR Spectra were recorded on a Pye Unicam Spectra-1000 (KBr disk). NMR spectra were recorded on a Varian 500 MHz spectrometer in (CD 3 ) 2 SO using Si(CH 3 ) 4 as an internal standard. Elemental analyses were obtained from the Micro-analytical Data Center at Cairo University, Egypt.…”

“…[3] In spite of the known efficacy of Tiazofurin, its high toxicity and lack of specificity represent a problem for its clinical use. [4] For this reason, many Tiazofurin analogues were synthesized aiming to produce derivatives with reduced toxicity. [5] As a part of our recent program directed toward syntheses of catabolically stable nucleoside analogues, we have recently reported on the synthesis and antiviral activity of a number of heterocyclic thioglycosides that have an interesting cytotoxic activity such as pyridine thioglycosides, [6] pyrimidine thioglycosides, [7] imidazole thioglycosides, [8] oxadiazole thioglycosides, [9] thiophene thioglycosides, [10] quinoline thioglycosides, [11] and thienopyrazole thioglycosides.…”

Identification of potent human carbonic anhydrase IX inhibitors: a combination of pharmacophore modeling, 3D-QSAR, virtual screening and molecular dynamics simulations

“…The topmost 30 ligands, having Glide energies in the range from À64.97 to À37.74 kcal mol À1 were selected. One interesting observation that should be mentioned here is that, among the shortlisted ligands, one ligand, ZINC003813042, also known as acetazolamide, is the bound inhibitor of our target protein hCA IX (PDB ID: 3IAI) and two ligands, ZINC004217560 and ZINC058660702, commonly known as tiazofurin and pevonedistat, respectively, are well-known anticancer agents (Popsavin et al, 2016;Swords et al, 2018;Vitale et al, 1997). The fact that we obtained the bound inhibitor and known anticancer agents as hits from the drug library indicates that our methodology of virtual screening to predict new hCA IX inhibitors is apt.…”

In Vitro Inhibition Effects of 2-Amino Thiazole Derivatives on Lactoperoxidase Enzyme Activity

“…For the thiazole ring system, antimicrobial [7,8], antiviral [9], antiprotozoal [10], anticancer [11], antioxidant [12], anticonvulsant [13], antidiabetic [14], antihypertensive [15], anticholinesterase [16,17], analgesic and anti-inflammatory [18] activities have been reported.…”