Abstract
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.
Mini-Reviews in Medicinal Chemistry
Title:New 1-phthalazinone Scaffold based Compounds: Design, Synthesis, Cytotoxicity and Protein Kinase Inhibition Activity
Volume: 18 Issue: 20
Author(s): Nehad E. Abo-elmagd, Riham F. George, Manal A. Ezzat and Reem K. Arafa*
Affiliation:
- University of Science and Technology, Zewail City of Science and Technology, Cairo, 12588,Egypt
Keywords: Cytotoxicity, EGFR, 1-Phthalazinone, VEGFR-2, xenograft, Cancer.
Abstract: 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).
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Cite this article as:
Abo-elmagd E. Nehad , George F. Riham , Ezzat A. Manal and Arafa K. Reem *, New 1-phthalazinone Scaffold based Compounds: Design, Synthesis, Cytotoxicity and Protein Kinase Inhibition Activity, Mini-Reviews in Medicinal Chemistry 2018; 18 (20) . https://dx.doi.org/10.2174/1389557518666180903153254
DOI https://dx.doi.org/10.2174/1389557518666180903153254 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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