Quinazolinone Platinum Metal Complexes: in silico Design, Synthesis and Evaluation of Anticancer Activity

Sanjay D. Sawant*, Megha Sahu and Amit G. Nerkar

Department of Pharmaceutical Chemistry, Sinhgad Technical Education Society's, Smt. Kashibai Navale College of Pharmacy, Kondhwa (Bk), Pune-411 048, India

*Corresponding author: E-mail: principal.skncop@sinhgad.edu


Dihydrofolate reductase (DHFR) has been explored as a target for the development of agents for wide variety of human diseases, including cancer, autoimmune and infectious diseases. Several metal complexes are being used in management of cancer. The square planar Pt(II) complex, cis PtCl2(NH3)2 turned out to be even more effective at forcing filamentous growth. Cisplatin is an inorganic heavy metal complex that has activity similar to cell-cycle-phase-nonspecific alkylating agents such as cyclophosphamide and some other Ni and Cu metal complexes. It produces intrastrand DNA cross-link and form DNA adducts, thus inhibiting the synthesis of DNA, RNA and proteins preferentially. in silico Screening of platinum metal complexes was performed by Vlife MDS 4.3 software. In this procedure, selection of molecule, selection of PDB, optimization of PDB and docking of molecules was carried out. Synthesis of metal complexes was done by multi component reaction method. Platinum metal complexes of quinazolinone Schiff bases prioritized by in silico studies were characterized by IR, TLC, NMR, XRD, FESEM and some physico-chemical parameters. Prioritized molecules were further evaluated by in vitro anticancer cell line assay on ten cell lines with adriamycin as standard. The results showed that the platinum metal complexes of qunazolinone Schiff bases can be potential anticancer agents through DHFR inhibitory mechanism.


Platinum, Dihydrofolate reductase, Cisplatin, Autoimmune disease, Methotrexate.

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