115754-65-9Relevant academic research and scientific papers
Quinazolinone platinum metal complexes: In silico design, synthesis and evaluation of anticancer activity
Sawant, Sanjay D.,Sahu, Megha,Nerkar, Amit G.
, p. 2164 - 2170 (2018/09/10)
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.
Design and synthesis of quinazolinone tagged acridones as cytotoxic agents and their effects on EGFR tyrosine kinase
Babu, Yarlagadda Rajesh,Bhagavanraju, Mantripragada,Reddy, Gade Deepak,Peters, Godefridus J.,Prasad, Velivela V. S. Rajendra
, p. 624 - 634 (2014/11/08)
In a quest for finding potent cytotoxic molecules, we have designed and synthesized a new scaffold by tagging quinazolinones with an acridone moiety. The new acridone-4-carboximide derivatives were evaluated for their cytotoxic potentials against the MCF7 breast cancer cell line and three colon cancer cell lines (LS174T, SW1398, and WiDr). Compound 26 showed relatively potent cytotoxic activity among the derivatives, against all the cell lines tested. Mechanistic studies for the selected derivatives 7, 8, 16, 17, 25, and 26 were conducted through in vitro EGFR tyrosine kinase inhibition studies. The results indicate that compound 26 has a better EGFR tyrosine kinase inhibitory profile. The in vitro EGFR inhibition data was correlated with the cytotoxic properties, and molecular docking studies were performed with regard to the receptor autophosphorylation sites of the protein kinase domain of the EGFR.
Synthesis and antiviral activity of 2-aryl-3-(substituted-benzalamino)- 4(3H)-quinazolinones
Pandey, Shradha,Singh, Pravin K.,Siddiqui,Singh, Jagdamba
, p. 835 - 839 (2012/04/04)
A series of new heterocyclic compounds 2-aryl-3-(substituted-benzalamino)- 4(3H)-quinazolinone have been synthesized by the treatment of 3-amino-2-aryl-4(3H)-quinazolinone with a substituted benzaldehyde in ethanol. All the synthesized compounds were char
Synthesis, antitubercular and anticancer activities of substituted furyl-quinazolin-3(4H)-ones
Raghavendra, Nulgulmnalli M.,Thampi, Parameshwaran,Gurubasavarajaswamy, Purvarga M.,Sriram, Dharmarajan
, p. 635 - 641 (2008/12/21)
Some novel substituted-3-{[(1E)-(substituted-2-furyl)-methylene]amino} quinazolin-4(3H)-one (5, 6, 7) a-f were synthesized by a multi-step process. These synthesized compounds are characterized by various spectroscopic techniques and evaluated for their antitubercular and anticancer activities. Biological activity indicated that some of the title compounds are potent antitubercular and anticancer agents.
Synthesis of some new aziridine derivatives
Deshmukh,Chavan, Smt P. B.
, p. 471 - 474 (2007/10/03)
Oxidation of 3-amino-6-bromo-2-phenylquinazolin4(3H)-one (2) with lead tetraacetate at - 20°C gives 3-acetoxyamino-6-bromo-2-phenylquinazolin-4( 3 H )-one (3) which selectively aziridinates the olefinic esters to yield methyl/ethyl 1 -[6-bromo-4(3H)-oxo-2
