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

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2020年 / 53卷 / 10期

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

页码：895 / 898

页数：4

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