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.
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