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

被引:10
|
作者
Zykova, S. S. [1 ,2 ]
Kizimova, I. A. [2 ]
Syutkina, A. I. [2 ]
Toksarova, Yu. S. [2 ]
Igidov, N. M. [2 ]
Ibishov, D. F. [3 ]
Boichuk, S. V. [4 ]
Dunaev, P. D. [4 ]
Galembikova, A. R. [4 ]
Korochkina, R. R. [5 ]
机构
[1] Perm Mil Inst Troops Natl Guard Russian Federat, 1 Gremyachii Log St, Perm 614112, Russia
[2] Perm State Pharmaceut Acad, Minist Hlth Russian Federat, 2 Polevaya St, Perm 614990, Russia
[3] Academician DN Pryanishnikov Perm State Agr Techn, 123 Petropavlovskaya St, Perm 614000, Russia
[4] Kazan State Med Univ, 49 Butlerov St, Kazan 4230012, Russia
[5] RE Plekhanov Russian State Econ Univ, Moscow, Russia
基金
俄罗斯科学基金会;
关键词
2-amino-5-substituted derivatives of 4; 5-dihydro-1H-pyrrole-3-carboxulate; MTT test; acute toxicity; cytotoxicity; GIST T-1 tumor cell line; CHEMISTRY; RECYCLIZATION;
D O I
10.1007/s11094-020-02096-z
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:895 / 898
页数:4
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