Synthesis and Cytotoxic Evaluation of Novel 3-Substituted Derivatives of 2-Indolinone

Authors

  • Farzad Kobarfard Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran. Pharmaceutical Research Sciences Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran. Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
  • Mahmoud Mosaddegh Traditional Medicine and Materia Medica Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
  • Maryam Hamzeloo Moghadam Traditional Medicine and Materia Medica Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
  • Saeideh Ghafari Traditional Medicine and Materia Medica Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran
  • Shaya Mokhtari Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran. Student Research Committee, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
  • Zohreh Soleymani Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Abstract:

     The assessment of the degree or rate of cellular proliferation and cell viability is critical for the assessment of the effects of drugs on both normal and malignant cell populations. In the present study, a few novel 3-substituted derivatives of 2-indolinones were synthesized by condensation of substituted oxindole or isatin derivatives with appropriate aldehydes or primary aromatic amines respectively. The synthesized compounds were screened for their cytotoxicity against HT-29 (human colon adenocarcinoma cell line) and MCF-7 (human breast adenocarcinoma cell line) cells using short term cytotoxicity MTT assay protocol. A few derivatives with IC50 < 10 μM were identified among them. The compound bearing 5-bromo substitution was the most potent derivative. Global physicochemical properties for compounds IVa-e and Va-h were calculated and the two most active compounds (IVa and IVb) showed similar Clog P-values.  

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Journal title

volume 11  issue 2

pages  411- 421

publication date 2012-05-23

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