2. Academic Validation
  3. Bis-isatin hydrazones with novel linkers: Synthesis and biological evaluation as cytotoxic agents

Bis-isatin hydrazones with novel linkers: Synthesis and biological evaluation as cytotoxic agents

  • Eur J Med Chem. 2016 Jan 27:108:415-422. doi: 10.1016/j.ejmech.2015.11.047.
Hany S Ibrahim 1,  Sahar M Abou-Seri 2,  Nasser S M Ismail 3,  Mahmoud M Elaasser 4,  Mohamed H Aly 5,  Hatem A Abdel-Aziz 6
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Egyptian Russian University, Badr City, Cairo 11829, Egypt.
  • 2 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo 11562, Egypt. Electronic address: saharshaarawy_69@yahoo.com.
  • 3 Pharmaceutical Chemistry Department, Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University, Cairo 12311, Egypt.
  • 4 The Regional Center for Mycology and Biotechnology, Al-Azhar University, Cairo, Egypt.
  • 5 Department of Pharmacology and Toxicology, Faculty of Pharmacy, British University in Egypt (BUE), Cairo, Egypt; Department of Biology, School of Sciences and Engineering (SSE), The American University in Cairo, 11835 New Cairo, Egypt.
  • 6 Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia; Department of Applied Organic Chemistry Department, National Research Center, Dokki, Cairo 12622, Egypt. Electronic address: hatem_741@yahoo.com.
PMID: 26706352 DOI: 10.1016/j.ejmech.2015.11.047
Abstract

Many bis-isatins and isatins with hydrazide extension were reported to have a potential anti-proliferative effects against different Cancer cell lines and Cancer targets. In this study, four series of bis-isatins with hydrazide linkers were synthesized. These compounds were investigated for their antitumor activity by assessing their cytotoxic potency against HepG2, MCF-7 and HCT-116 Cancer cell lines. Compound 21c possessed significant cytotoxic activity against MCF-7 (IC50 = 1.84 μM) and HCT-116 (IC50 = 3.31 μM) that surpasses the activity of doxorubicin against both cell lines (MCF-7; IC50 = 2.57 μM and HCT-116; IC50 = 3.70 μM). Cell cycle analysis and annexin V-FITC staining of MCF-7 cells treated with 21c suggested that the cytotoxic effect of the compound could be attributed to its pro-apoptotic activity.

Keywords

Bis-isatin hydrazones; Cell cycle; Cytotoxic; Pro-apoptotic.

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