Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

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Abstract

An efficient synthesis of some new 1,4-disubstituted phthalazine derivatives and their anticancer activity

Author(s): Ashraf Farouk Wasfy, Aly Abdelmaboud Aly and Mohamed Sayed Behalo and Nora Sobhi Mohamed

A novel series of phthalazine derivatives bearing isoindol-1,3-dione moiety were synthesized by treating ethyl{4-[4- (1,3-dioxo-1,3-dihydroisoindole-2-yl)-phenyl] phthalazin-1-yloxy}acetate (3) and {4-[4-(1,3-Dioxo-1,3- dihydroisoindol-2-yl)phenyl]phthalazin-1-yloxy} acetic acid hydrazide (7a) with various chemical reagents.The newly synthesized compounds were characterized on the basis of their spectral (1H NMR, 13C NMR, Ms, IR) analyses. In vitro, most of the synthesized derivatives were screened for their antitumor activity against MCF-7 cells using MTT assay. Compounds 16b, 18, 13, 15, 17 showed the most potent cytotoxic effect concluded from their IC50 values 50, 70, 150, 180 and 100 μg/ml respectively


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