- Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives
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Some new 3H-quinazolin-4-one derivatives were synthesised and screened for anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities. Compound 15d was more potent in reducing the cell viabilities of HT-29 and SW620 cells lines to 38%, 36.7%, compared to 5-FU which demonstrated cell viabilities of 65.9 and 42.7% respectively. The IC50 values of 15d were ~20?μg/ml. Assessment of apoptotic activity revealed that 15d decreased the cell viability by down regulating Bcl2 and BclxL. Moreover, compounds, 8j, 8d/15a/15e, 5b, and 8f displayed lowered IC50 values than oleanolic acid against proinflammatory isoforms of hGV, hG-X, NmPLA2, and AmPLA2. In addition, 8d, 8h, 8j, 15a, 15b, 15e, and 15f showed better anti-α-amylase than quercetin, whereas 8g, 8h, and 8i showed higher anti-α-glucosidase activity than allopurinol. Thus, these compounds can be considered as potential antidiabetic agents. Finally, none of the compounds showed higher antiproteases or xanthine oxidase activities than the used reference drugs.
- El-Sayed, Nahed N. E.,Almaneai, Norah M.,Ben Bacha, Abir,Al-Obeed, Omar,Ahmad, Rehan,Abdulla, Maha,Alafeefy, Ahmed M.
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p. 672 - 683
(2019/04/02)
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- Quinazoline clubbed 1,3,5-triazine derivatives as VEGFR2 kinase inhibitors: design, synthesis, docking, in vitro cytotoxicity and in ovo antiangiogenic activity
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Abstract: A series of quinazoline clubbed 1,3,5-triazine derivatives (QCT) were synthesized and evaluated for their in vitro anticancer activity against HeLa (human cervical cancer), MCF-7 (human breast cancer cell), HL-60 (human promyelocytic leukemia cell), HepG2 (human Hepatocellular carcinoma cell), and one normal cell line HFF (human foreskin fibroblasts). In vitro assay result encouraged to further move towards in ovo anticancer evaluation using chick embryo. The series of QCT derivatives showed higher anticancer and antiangiogenic activity against HeLa and MCF-7 cell lines. In the series, synthetic molecule 8d, 8l, and 8m displayed significant activity. Further, these results substantiated by docking study on VGFR2. SAR study concluded that the potency of drugs depends on the nature of aliphatic substitution and the heterocyclic ring system. Graphical Abstract: [Figure not available: see fulltext.]
- Pathak, Prateek,Shukla, Parjanya Kumar,Kumar, Vikas,Kumar, Ankit,Verma, Amita
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- Quinazolinone platinum metal complexes: In silico design, synthesis and evaluation of anticancer activity
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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.
- Sawant, Sanjay D.,Sahu, Megha,Nerkar, Amit G.
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p. 2164 - 2170
(2018/09/10)
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- Design and synthesis of quinazolinone tagged acridones as cytotoxic agents and their effects on EGFR tyrosine kinase
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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.
- Babu, Yarlagadda Rajesh,Bhagavanraju, Mantripragada,Reddy, Gade Deepak,Peters, Godefridus J.,Prasad, Velivela V. S. Rajendra
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p. 624 - 634
(2014/11/08)
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- 2-{2"-carbomyl-5"-[3′-amino-2′-methylmono/ dihalosubstituted quinazolin-4′(3'h)-onomethylene]- 1",3",4"-oxadiazol-2"-yl}-4,5-dihydroimidazolines as potential antihypertensive agents
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Twelve new 2- {2"-carbomyl - 5" - [3′-amino-2′ - methylmono / dihalosubstituted quinazolin- 4′ (3'H) - onomethylene] - 1",3",4" - oxadiazol-2"-yl} -4, 5- dihydroimidazolines were prepared and evaluated for their cardiovascular activity. The most active compound of this series is 2-{2"- carbomyl-5"-[3′-amino-2′-methyl-6-bromoquinazolin-4′(3'H)-onomethylene]-",3",4"-oxadiazol-2"- yl}-4,5-dihydroimidazolines i.e. compound VIc.
- Tyagi, Mirdula
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p. 713 - 721
(2015/01/16)
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- Synthesis and antiviral bioactivities of 2-aryl- or 2-methyl-3- (substituted- benzalamino)-4(3H)-quinazolinone derivatives
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A simple and general method has been developed for the synthesis of various 4(3H)-quinazolinone derivatives by the treatment of the appropriate 3-amino-2-aryl-4(3H)-quinazolinone with a substituted benzaldehyde in ethanol. The structures of the compounds were characterized by elemental analysis, IR, 1H-NMR and 13C-NMR spectra. The title 2-aryl- or 2-methyl-3-(substituted-benzalamino)-4(3H)-quinazolinone compounds III-1-III-31 were found to possess moderate to good antiviral activity. Semi-quantitative PCR and Real Time PCR assays were used to ascertain the target of action of compound III-31 against TMV. The studies suggest that III-31 possesses antiviral activity due to induction of up-regulation of PR-1a and PR-5, thereby inhibiting virus proliferation and movement by enhancement of the activity of some defensive enzyme.
- Gao, Xingwen,Cai, Xuejian,Yan, Kai,Song, Baoan,Gao, Lili,Chen, Zhuo
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p. 2621 - 2642
(2008/03/18)
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- Synthesis, antitubercular and anticancer activities of substituted furyl-quinazolin-3(4H)-ones
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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.
- Raghavendra, Nulgulmnalli M.,Thampi, Parameshwaran,Gurubasavarajaswamy, Purvarga M.,Sriram, Dharmarajan
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p. 635 - 641
(2008/12/21)
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- Quinazolin-4-one derivatives
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A medicament having an inhibitory activity against hematopoietic prostaglandin D2 synthase, which comprises as an active ingredient a compound represented by the following general formula (I) or a salt thereof: wherein X represents a group represented by the formula —N═C(R5)— or the formula —NH—CH(R5)—, R1, R2, R3, and R4 represent a hydrogen atom, a halogen atom, a C1 to C6 alkyl group, or a hydroxy group, R5 represents a C1 to C6 alkyl group or a C6 to C10 aryl group, and R represents an amino group.
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Page/Page column 29
(2010/11/24)
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- Synthesis of Quinazolinylpyrimidinediones and Their Anti-inflammatory Activity
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Hexahydro-1--3-aryl-2-thioxopyrimidine-4,6-diones (IV) have been prepared and converted into hexahydro-1--3-aryl-5-benzyliden-2-thioxopyrimidine-4,6-diones (V) and hexahydro-1-2-alkyl-4(
- Kumar, Atul,Singh, S.,Saxena, A. K.,Shanker, K.
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p. 443 - 447
(2007/10/02)
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- Synthesis and Pharmacological Activity of Some New 4(3H)-Quinazolone Derivatives
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New derivatives of 2-methyl-4(3H)-quinazolone have been prepared and their structures assigned on the basis of IR, PMR and mass spectra.Some of them show CNS depressant activity.
- Ossman, Abdel Rahman El Nasser,Safwat, H. M.,Aziza, Mohsen A.
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p. 333 - 335
(2007/10/02)
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