2. Academic Validation
  3. Synthesis and cytotoxic activities of some pyrazoline derivatives bearing phenyl pyridazine core as new apoptosis inducers

Synthesis and cytotoxic activities of some pyrazoline derivatives bearing phenyl pyridazine core as new apoptosis inducers

  • Eur J Med Chem. 2016 Apr 13:112:48-59. doi: 10.1016/j.ejmech.2016.01.048.
Riham F George 1,  Marwa A Fouad 2,  Iman E O Gomaa 3
Affiliations

Affiliations

  • 1 Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, El-kasr Elaini Street, Cairo 11562, Egypt. Electronic address: rihamfgeorge@yahoo.com.
  • 2 Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, El-kasr Elaini Street, Cairo 11562, Egypt.
  • 3 Biotechnology Sector, Faculty of Pharmacy and Biotechnology, German University in Cairo (GUC), New Cairo City, Egypt.
PMID: 26874744 DOI: 10.1016/j.ejmech.2016.01.048
Abstract

The cyclization of Chalcones 3a-3u with 3-hydrazinyl-6-phenylpyridazine 7 under basic condition led to the formation of new pyrazoline derivatives 8a-8u. All final compounds were characterized by spectral and elemental analyses. They were screened for their antiproliferative activities against A549 (lung), HepG-2 (liver), CaCo-2 (intestinal) and MCF-7 (breast) Cancer cell lines. Some of the synthesized compounds exhibited promising antiproliferative activities especially compound 8k with IC50 values of 8.33, 1.67 and 10 μM against HepG-2, MCF-7 and CaCo-2 Cancer cell lines, respectively. Moreover, their antiproliferative activity was due to Apoptosis rather than necrosis induction except compound 8h which exhibited equal apoptotic and necrotic properties. Compound 8k showed 5 fold increase in Caspase-3 activity indicating that the Apoptosis proceeds via Caspase-3 activation.

Keywords

Apoptosis; Caspase-3; Chalcones; MTT assay; Pyrazolylpyridazines.

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