Abstract
Several nitrogen heterocycles are considered as privileged scaffolds in drug discovery and are present in several drugs with diverse biological activities. Herein, we report the synthesis and characterization of phthalazinone derivatives by using a green synthesis protocol under microwave irradiation. The reduced reaction time and high yield are some of the advantages that render this procedure a greener alternative to conventional chemical synthesis. The structures of all new derivatives were confirmed by spectral analysis. Synthesized derivatives show an effective antimicrobial effect. These compounds were also screened for their in vitro anticancer activity against colon cancer cell line (HCT116). Among the synthesized derivatives are exhibited the highest anticancer activity with IC50 of 28.97±0.11, 66.25±0.14 and 76.04±0.09 μM respectively. The antiproliferative activity was supported by molecular docking studies that showed that phthalazinone derivatives would potentially act through inhibition of PARP. The simulation studies substantiated the biological results as an active compounds in term of binding interactions and scores.
Preparation series of phthalazinone derivatives by using a green protocol synthesis under microwave irradiations. Synthesized derivatives show an effective inhibit the antimicrobial and anticancer activity against a colon cancer cell line. The antiproliferative activity was supported with molecular docking studies that showed that phthalazinone derivatives are potentially act through inhibition of PARP.