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Pharmaceutical Chemistry Journal

, Volume 53, Issue 10, pp 895–898 | Cite as

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

  • S. S. ZykovaEmail author
  • 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
Article

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.

Keywords

2-amino-5-substituted derivatives of 4,5-dihydro-1H-pyrrole-3-carboxulate MTT test acute toxicity cytotoxicity GIST T-1 tumor cell line 

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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2020

Authors and Affiliations

  • S. S. Zykova
    • 1
    • 2
    Email author
  • I. A. Kizimova
    • 2
  • A. I. Syutkina
    • 2
  • Yu. S. Toksarova
    • 2
  • N. M. Igidov
    • 2
  • D. F. Ibishov
    • 3
  • S. V. Boichuk
    • 4
  • P. D. Dunaev
    • 4
  • A. R. Galembikova
    • 4
  • R. R. Korochkina
    • 5
  1. 1.Perm Military Institute of Troops of the National Guard of the Russian FederationPermRussia
  2. 2.Perm State Pharmaceutical AcademyMinistry of Health of the Russian FederationPermRussia
  3. 3.Academician D. N. Pryanishnikov Perm State Agrarian Technological UniversityPermRussia
  4. 4.Kazan State Medical UniversityKazanRussia
  5. 5.R. E. Plekhanov Russian State Economics UniversityMoscowRussia

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