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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Research Article

New 1-phthalazinone Scaffold based Compounds: Design, Synthesis, Cytotoxicity and Protein Kinase Inhibition Activity

Author(s): Nehad E. Abo-elmagd, Riham F. George, Manal A. Ezzat and Reem K. Arafa*

Volume 18, Issue 20, 2018

Page: [1759 - 1774] Pages: 16

DOI: 10.2174/1389557518666180903153254

Price: $65


Background & Method: A series of thirty-one new 1-phthalazinones was designed and synthesized based on the well-known VEGFR inhibitor vatalanib. The obtained phthalazinones were screened for their cytotoxic activity against DLD-1 and LoVo (colon), and Panc-1 and Paca-2 (pancreas) cancer cell lines using MTT assay. The tested compounds revealed exceptionally promising cytotoxic activity against LoVo cell lines with IC50 ranges 0.18-780 nM.

Conclusion: Finally, these compounds were also found to be dual inhibitors of VEGFR-2 and EGFR in the in vitro enzyme assay with higher potency against the former (IC50 = 0.023-0.41 nM).

Keywords: Cytotoxicity, EGFR, 1-Phthalazinone, VEGFR-2, xenograft, Cancer.

Graphical Abstract

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