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Synthesis and Cytostatic Activity of (E)-Ethyl-2-Amino-5-(3,3-Dimethyl-4-Oxobutyliden)-4-Oxo-1- (2-Phenylaminobenzamido)-4,5-Dihydro-1Hpyrrol-3-Carboxylate

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Synthesis and Cytostatic Activity of (E)-Ethyl-2-Amino-5-(3,3-Dimethyl-4-Oxobutyliden)-4-Oxo-1- (2-Phenylaminobenzamido)-4,5-Dihydro-1Hpyrrol-3-Carboxylate

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S. S. Zykova, I. A. Kizimova, A. I. Syutkina, Yu. S. Toksarova, N. M. Igidov, D. F. Ibishov, S. V. Boichuk, P. D. Dunaev, A. R. Galembikova & R. R. Korochkina 

Interaction of (Z)-N-(5-tert-butyl)-2-oxofuran-3(2H)-yliden-2-phenylaminobenzohydrazide (I) with cyanoacetic ester in the presence of triethylamine was used to synthesize the novel derivative (E)-ethyl-2-amino-5-(3,3-dimethyl-4-oxobutyliden)-4-oxo-1-(2-phenylaminobenzamido)-4,5-dihydro-1H-py rrole-3-carboxylate (II). The acute toxicity of this compound was studied, along with its cytotoxic activity against gastrointestinal stromal tumor (GIST) cell line T-1. Compound II showed a concentration- and time-dependent effect comparable with the antitumor compounds imatinib, paclitaxel, etoposide, and hydroxyurea.

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Year 2020
Language English
Format PDF
DOI 10.1007/s11094-020-02096-z