1417577-17-3Relevant academic research and scientific papers
Efficient synthesis and cell migration inhibitory effect of substituted benzamidothiazolylpyrazole-capped AWD*I-NH2
Chen, Jun,Li, Qiqi,Liao, Xing-Hua,Peng, Wancai,Shao, Hui,Takada, Yoshikazhu,Tang, Guanping,Yang, Mian,Ye, Long,Zhang, Tong-Cun
, (2020)
Substituted (2-benzamidothiazol-5-yl)pyrazole-capped AWD*I-NH2 were synthesized and their antimigration activity was studied. The improved efficiency and scalability of the analog synthesis was achieved via a late-stage diversification of the benzoyl group and a convergent route in which the bisazole capping agents and off-resin peptide AWD*I-NH2 were prepared in parallel and coupled together in solution at the last step. Bioassay results indicate that all the peptidomimetics can significantly inhibit the migration of breast cancer cells MDA-MB-231 but possess no apparent cytotoxicity. In general, the antimigration potency of the peptidomimetics is correlated to the electron-withdrawing capacity of the substituents on the terminal phenyl ring. The inhibitory effect shows dose-dependent and holds also against lung and cervical cancer cells. The level of f-actin was reduced dramatically in cells treated with the inhibitor, suggesting that the migration inhibitory effect is related to the disruption of cell locomotive protrusions.
Ester-based pyrazole bithiazole amine compound as well as preparation method and application thereof
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, (2020/09/12)
The invention discloses an ester-based pyrazole bithiazole amine compound as well as a preparation method and application thereof. The structural general formula of the ester-based pyrazole bithiazoleamine compound is shown in the specification. The compound is a double-five-membered nitrogen heterocyclic bifunctional compound, is convenient for realizing high-throughput synthesis and diversifiedderivation of thiazole amine and pyrazole, and can be widely applied to the research, development and production of thiazole bipyrazole drugs.
