1264191-95-8Relevant academic research and scientific papers
A facile one-pot, three-component synthesis of a new series of thiazolyl pyrazole carbaldehydes: In vitro anticancer evaluation, in silico ADME/T, and molecular docking studies
Mamidala, Srikanth,Aravilli, R Kowshik,Ramesh, Gondru,Khajavali, Shaik,Chedupaka, Raju,Manga, Vijjulatha,Vedula, Rajeswar Rao
, (2021/04/09)
A series of thiazolyl pyrazole carbaldehydes (4a-n) were synthesized by conventional method using thiosemicarbazide, substituted phenacyl bromides, substituted 3-acetylcoumarins, and Vilsmeyer-Hack reagent. Structures of all the synthesized compounds were confirmed by spectral (1H & 13C NMR, FTIR, Mass) and analytical data. The target compounds were screened for their in vitro anticancer activity. From the results, it was found that the compound 4m has shown significant antiproliferative activity against all tested cell-lines. Furthermore, in silico ADME/T profiles were also carried out to set effective lead candidates for the future anticancer drug discovery initiatives. Molecular docking studies were carried out against colchicine binding site of β-tubulin and the results were in concordance with the in vitro anticancer data.
Synthesis and biological evaluation of novel 2,4-disubstituted-1,3- thiazoles as anti-Candida spp. agents
Chimenti, Franco,Bizzarri, Bruna,Bolasco, Adriana,Secci, Daniela,Chimenti, Paola,Granese, Arianna,Carradori, Simone,D'Ascenzio, Melissa,Lilli, Daniela,Rivanera, Daniela
experimental part, p. 378 - 382 (2011/02/25)
A new series of [4-(4′-substituted-phenyl)thiazol-2-yl]hydrazine derivatives were synthesized in good yield (86-99%) and characterized by elemental analysis, IR, 1H NMR, and mass spectral studies. The compounds were assayed for their in vitro broad-spectrum antifungal activity, compared to clotrimazole and fluconazole, against 20 clinical isolates of pathogenic Candida spp., representing five different species. The results showed that the presence of heterocyclic or bicyclic rings on hydrazone moiety in position C2 of thiazole revealed a promising selective inhibitory activity especially against Candida albicans and Candida glabrata.
