Staff Members - Benha University
An efficient synthesis of some new 1,4-disubstituted phthalazine derivatives and their anticancer activity
Der Pharma Chemica • 2013
Publication Information
Authors
Ashraf Farouk Wasfy*, Aly Abdelmaboud Aly and Mohamed Sayed Behalo and
Nora Sobhi Mohamed*
Keywords
Phthalazin-1-(2H)-One; Acid hydrazide, Isoindol-1,3-dione; Antitumor activity
Journal
Der Pharma Chemica
Publisher
Not Available
Volume
5
Issue
2
Pages
82-96
publication.type
International
Paper Link
Not Available
Supplementary Materials
Not Available
Abstract
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.
(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.