电邮这篇文章 Synthesis and Biological Activity of 2-amino-1-aryl-5-(3,3-dimethyl-2-oxobutylidene)-4-oxo-N-(thiazol-5-yl)-4,5-dihydro-1h-pyrrole-3-carboxamides
- 作者: Zykova S.S.1, Igidov N.M.2, Zakhmatov A.V.2, Kiselev M.A.2, Galembikova A.R.3, Khusnutdinov R.R.3, Dunaev P.D.3, Boichuk S.V.3, Chernov I.N.4, Rodin I.A.5
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隶属关系:
- Perm Federal Penitentiary Service Institute
- Perm State Pharmaceutical Academy
- Kazan State Medical University
- Research Institute of Chemistry, N. I. Lobachevsky State University of Nizhny Novgorod
- I. T. Trubilin Kuban State Agrarian University
- 期: 卷 52, 编号 3 (2018)
- 页面: 198-204
- 栏目: Search for New Drugs
- URL: https://bakhtiniada.ru/0091-150X/article/view/245076
- DOI: https://doi.org/10.1007/s11094-018-1790-9
- ID: 245076
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详细
A series of new 2-aminopyrrole derivatives [2-amino-1-aryl-5-(3,3-dimethyl-2-oxobutylidene)-4-oxo-N-(thiazol-5-yl)-4,5-dihydro-1H-pyrrole-3-carboxamides IIa-h] were synthesized via the reaction of 4-arylamino-2-tert-butyl-2,5-dihydro-5-oxofuran-2-ylacetates (Ia-h) with 2-cyano-N-(thiazol-2-yl)acetamide in the presence of Et3N. Studies of the biological activity of the synthesized compounds found that they possessed low toxicity and that 2-amino-1-(2-bromophenyl)-5-(3,3-dimethyl-2-oxobutylidene)-4-oxo-N-(thiazol-5-yl)-4,5-dihydro-1H-pyrrole-3-carboxamide (IIb) and 2-amino-1-(2,4-dichlorophenyl)-5-(3,3-dimethyl-2-oxobutylidene)-4-oxo-N-(thiazol-5-yl)-4,5-dihydro-1H-pyrrole-3-carboxamide (IIg) exhibited radical-binding activity greater than that of trolox and cytotoxic activity against gastrointestinal stromal tumor (GIST) cells, including those resistant to the target drug imatinib (Glivec). The cytotoxic activity of the synthesized compounds was comparable with that of doxorubicin chemotherapeutics and exceeded significantly those of etoposide, paclitaxel, and hydroxyurea. Apossible molecular mechanism of action of the synthesized compounds might be their ability to disrupt cell division and induce selective accumulation of M-phase cells with subsequent death by a mitotic catastrophe pathway.
作者简介
S. Zykova
Perm Federal Penitentiary Service Institute
编辑信件的主要联系方式.
Email: zykova.sv@rambler.ru
俄罗斯联邦, 125 Karpinskogo St., Perm, 614012
N. Igidov
Perm State Pharmaceutical Academy
Email: zykova.sv@rambler.ru
俄罗斯联邦, 2 Polevaya St., Perm, 614099
A. Zakhmatov
Perm State Pharmaceutical Academy
Email: zykova.sv@rambler.ru
俄罗斯联邦, 2 Polevaya St., Perm, 614099
M. Kiselev
Perm State Pharmaceutical Academy
Email: zykova.sv@rambler.ru
俄罗斯联邦, 2 Polevaya St., Perm, 614099
A. Galembikova
Kazan State Medical University
Email: zykova.sv@rambler.ru
俄罗斯联邦, 49 Butlerova St., Kazan, Tatarstan, 420012
R. Khusnutdinov
Kazan State Medical University
Email: zykova.sv@rambler.ru
俄罗斯联邦, 49 Butlerova St., Kazan, Tatarstan, 420012
P. Dunaev
Kazan State Medical University
Email: zykova.sv@rambler.ru
俄罗斯联邦, 49 Butlerova St., Kazan, Tatarstan, 420012
S. Boichuk
Kazan State Medical University
Email: zykova.sv@rambler.ru
俄罗斯联邦, 49 Butlerova St., Kazan, Tatarstan, 420012
I. Chernov
Research Institute of Chemistry, N. I. Lobachevsky State University of Nizhny Novgorod
Email: zykova.sv@rambler.ru
俄罗斯联邦, 23/5 Prosp. Gagarina, Nizhny Novgorod, 603950
I. Rodin
I. T. Trubilin Kuban State Agrarian University
Email: zykova.sv@rambler.ru
俄罗斯联邦, 13 Kalinina St, Krasnodar, 350044
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