• Archives of Pharmacal Research
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• 제26권7호
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• pp.511-515
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• 2003

Quinazolinones, 2-substituted and 3-substituted, mainly synthesized by microwave irradiation, were subjected to anti-platelet aggregation and inhibition of superoxide anion generation assays. Interestingly, 2-phenyl-4-quinazolinone (4) exhibited significant inhibitory activities toward platelet aggregation and neutrophil activation, and it might therefore serve as a prototype lead compound.

• Bulletin of the Korean Chemical Society
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• 제24권4호
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• pp.473-478
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• 2003

3-Amino-2-hydroxy-4(3H)-quinazolinone (3) was prepared via condensation of 1 with hydrazine hydrate. Treatment of 3 with appropriate acid in $POCl_3$, ethyl chloroacetate and activated olefinic compounds in DMF yielded the corresponding 3-(substituted)amino-2-hydroxy-4(3H)-quinazolinones 4, 5 and 6. The electron impact ionization mass spectra of compounds 3 and 4 show a weak molecular ion peak and a base peak of m/z 146 resulting from a cleavage fragmentation. The compounds 5 and 6 give a characteristic fragmentation pattern with a very stable fragment of benzopyrazolone (m/z 132).

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.251.2-251.2
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• 2003

The 2,3-trimethylene-4(3H)-quinazolinone and 2,3-tetramethylene-4(3H)-quinazolinone are not the only alkaloids isolated from plants. but are the part of a family of intriguing alkaloids including the bronchodilator vasicinone, anti-endotoxic isaindigotone, cytotoxic luotonins, antibiotic tryptanthrin, and antiinflammatory rutacearpine as well as related alkaloids. (omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.353.3-354
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• 2002

The reverse transriptase (RT) of HIV-1 is a proven target for inhibition of HIV-1 replication. Many nonnucleoside RT inhibitors (NNRTls) are in development stage for the clinical use: Among them. trovirdine (PETT). (thiophene) ethylpyridylthioureas (TET). and phenylethylpyridylureas (urea-PETT) are simple and flexible arylalkylarylureas. These are now considered to be very important as a potential therapeutics with remarkable antiviral activity against various mutant strains. (omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.250.2-250.2
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• 2003

A series of rutaecarpine homologues were prepared from 2,3-polymethylene-4(3H-quinazolinones in 4 steps [i) PhCHO/Ac$_2$O, ⅱ) O,$_3$ ⅲ) PhNHNH$_2$HCl, and ⅳ) PPA], in which dihedral angles of the two planar aromatic rings (indole and 4(3H)-quinazolinone) were controlled in a regular fashion. Their inhibitory activities on COX-1 and COX-2 were evaluated to show that the inhibitory activities were increased with the increase of the length of methylene unit while selectivities on COX-2 decreased leading a loss in trimethylene bridged system.

• 대한화학회지
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• 제61권4호
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• pp.157-162
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• 2017

In the present study, nanocrystalline mixed metal oxide, $CuMnO_3$ catalyst have been synthesized by mechanochemical method with green chemistry approach. The synthesized catalyst was characterized by analytical techniques including FTIR, XRD, SEM, TEM and BET surface area. The synthesized catalyst shows high surface area is $121.06m^2/g$ with particle size 18 nm. The one pot four component synthesis of substituted 2-phenyl-4(3H) quinazolinone from the reaction of anthranilic acid, benzoyl chloride, hydrazine hydrate and substituted benzaldehyde in presence of $CuMnO_3$ nanocatalyst has been carried out. It affords the corresponding products with high yield (76-95%) in very short reaction time. All the obtained products were characterized with $^1HNMR$, $^{13}CNMR$, FTIR and EIMS.

• Biomolecules & Therapeutics
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• 제27권5호
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• pp.492-501
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• 2019

Nitrogen-containing heterocycles such as quinoline, quinazolinones and indole are scaffolds of natural products and have broad biological effects. During the last years those structures have been intensively synthesized and modified to yield new synthetic molecules that can specifically inhibit the activity of dysregulated protein kinases in cancer cells. Herein, a series of newly synthesized isoquinolinamine (FX-1 to 8) and isoindoloquinazolinone (FX-9, FX-42, FX-43) compounds were evaluated in regards to their anti-leukemic potential on human B- and T- acute lymphoblastic leukemia (ALL) cells. Several biological effects were observed. B-ALL cells (SEM, RS4;11) were more sensitive against isoquinolinamine compounds than T-ALL cells (Jurkat, CEM). In SEM cells, metabolic activity decreased with $10{\mu}M$ up to 26.7% (FX-3), 25.2% (FX-7) and 14.5% (FX-8). The 3-(p-Tolyl) isoquinolin-1-amine FX-9 was the most effective agent against B- and T-ALL cells with IC50 values ranging from 0.54 to $1.94{\mu}M$. None of the tested compounds displayed hemolysis on erythrocytes or cytotoxicity against healthy leukocytes. Anti-proliferative effect of FX-9 was associated with changes in cell morphology and apoptosis induction. Further, influence of FX-9 on PI3K/AKT, MAPK and JAK/STAT signaling was detected but was heterogeneous. Functional inhibition testing of 58 kinases revealed no specific inhibitory activity among cancer-related kinases. In conclusion, FX-9 displays significant antileukemic activity in B- and T-ALL cells and should be further evaluated in regards to the mechanisms of action. Further compounds of the current series might serve as templates for the design of new compounds and as basic structures for modification approaches.