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：0
|
作者：
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
机构：
[1] Perm Military Institute of Troops of the National Guard of the Russian Federation,Perm State Pharmaceutical Academy
[2] Ministry of Health of the Russian Federation,undefined
[3] Academician D. N. Pryanishnikov Perm State Agrarian Technological University,undefined
[4] Kazan State Medical University,undefined
[5] R. E. Plekhanov Russian State Economics University,undefined
来源：
Pharmaceutical Chemistry Journal | 2020年 / 53卷
关键词：
2-amino-5-substituted derivatives of 4,5-dihydro-1; -pyrrole-3-carboxulate; MTT test; acute toxicity; cytotoxicity; GIST T-1 tumor cell line;
D O I：
暂无
中图分类号：
学科分类号：
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.
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页码：895 / 898
页数：3
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