On September 30, 2021, El-Dash, Yara; Elzayat, Emad; Abdou, Amr M.; Hassan, Rasha A. published an article.Recommanded Product: 2010-06-2 The title of the article was Novel thienopyrimidine-aminothiazole hybrids: Design, synthesis, antimicrobial screening, anticancer activity, effects on cell cycle profile, caspase-3 mediated apoptosis and VEGFR-2 inhibition. And the article contained the following:
A series of novel hybrid compounds of hexahydrobenzo[4,5]thieno[2,3-d]pyrimidine with aminothiazole scaffolds I (R = H, Br, O2N; R1 = H, Cl, Br; R2 = H, Me) were synthesized. The synthesized compounds were evaluated for their cytotoxic activity against the NCI-60 human tumor cell line panel. Compounds I (R = H; R1 = Cl; R2 = H) (II), I (R = Br; R1 = ; R2 = H) (III) and I (R = R1 = R2 = H) exhibited significant antiproliferative activities at 10-5 M dose. II exhibited excellent cytotoxic activity against CNS cancer cell lines including SNB-75 and SF-295 as well as renal cancer cell line CAKI-1 when compared with sorafenib as standard anticancer drug. In addition, III showed almost comparable anticancer activity to sorafenib against SNB-75 cell line and displayed moderate activity against SF-295 and CAKI-1 cell lines in comparison to sorafenib. II inhibited the vascular endothelial growth factor receptor 2 (VEGFR-2) with IC50 of 62.48 ± 3.7 nM and decreased both total VEGFR-2 and phosphorylated VEGFR-2 in treated SNB-75 cells suggesting its ability to down regulate cell proliferation, growth, and survival.. The flow cytometric anal. showed that II displayed its cytotoxic activity through the reduction of the cellular proliferation and induction of cell cycle arrest at the G2/M phase. II clearly boosted the level of the apoptotic caspase-3. All the synthesized compounds were also screened for their antibacterial and antifungal activity against four pathogenic strains of both Gram-pos. and Gram-neg. as well as Candida albicans. III exhibited antifungal activity against Candida albicans compared to nystatin as the standard antifungal compound The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Recommanded Product: 2010-06-2
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Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica