Hawas, Samia S.; El-Gohary, Nadia S.; Gabr, Moustafa T.; Shaaban, Mona I.; El-Ashmawy, Mahmoud B. published an article in 2019, the title of the article was Synthesis, molecular docking, antimicrobial, antiquorum-sensing and antiproliferative activities of new series of pyrazolo[3,4-b]pyridine analogs.Name: 4-Phenylthiazol-2-amine And the article contains the following content:
New series of pyrazolo[3,4-b]pyridines were prepared and evaluated for antimicrobial activity toward six selected microorganisms. Compounds and exhibited good activity toward Bacillus cereus. On the other hand, and evinced interesting activity over Candida albicans, whereas and displayed promising activity over Aspergillus fumigatus. Antiquorum-sensing effectiveness of the new members over Chromobacterium violaceum was also assessed, where compounds and exhibited higher activity than that of the reference compound, indole. In vitro antiproliferative assessment toward HepG2, HCT-116 and MCF-7 cancer cells evidenced that has notable effectiveness on all examined cell lines, whereas were active but to a lower extent. In vivo antitumor activity of and against EAC cells was also esteemed, where and showed considerable activity comparable to that of doxorubicin. Cytotoxicity screening over WI38 and WISH normal cells evinced that and are less cytotoxic than doxorubicin. Compounds and were evaluated for DNA-binding affinity and topoisomerase IIβ inhibitory activity. Analogs and illustrated strong DNA-binding affinity, whereas and exhibited interesting topoisomerase IIβ inhibitory activity. Compounds and were docked into topoisomerase IIβ, where showed preferential binding to topoisomerase IIβ. Computational studies articulated that the new members are in compliance with Veber’s standards and Lipinski’s rule. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Name: 4-Phenylthiazol-2-amine
The Article related to pyrazolo pyridine analog preparation antimicrobial antiquorum cancer topoisomerase, Pharmacology: Structure-Activity and other aspects.Name: 4-Phenylthiazol-2-amine
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica