314768-96-2Relevant academic research and scientific papers
GLUCOSE UPTAKE INHIBITORS
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Paragraph 01287; 01292-01294, (2020/01/24)
this invention provides compounds that modulate glucose uptake activity and cellular transport/uptake of glucose, and particularly GLUTS3, but also including but not limited to GLUT1-14 (SLC2A1-SLC2A14). Compounds of the invention are useful for treating diseases, including cancer, autoimmune diseases and inflammation, infectious diseases, and metabolic diseases.
Molecular modelling, synthesis, cytotoxicity and anti-tumour mechanisms of 2-aryl-6-substituted quinazolinones as dual-targeted anti-cancer agents
Hour,Lee,Chen,Lee,Zhao,Lee
, p. 1574 - 1586 (2013/08/23)
Background and Purpose Our previous study demonstrated that 6-(pyrrolidin-1-yl)-2-(3-methoxyphenyl)quinazolin-4-one (HMJ38) was a potent anti-tubulin agent. Here, HMJ38 was used as a lead compound to develop more potent anti-cancer agents and to examine t
2-Aryl-4-Quinazolinones And Their Pharmaceutical Compositions
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Paragraph 0086, (2013/05/08)
Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: wherein Ar represents R5, R6, R7, R8, R1′, R2′, R3′, R4
Synthesis and cytotoxicity of 6-pyrrolidinyl-2-(2-substituted phenyl)-4-quinazolinones
Hour, Mann-Jen,Yang, Jai-Sing,Lien, Jin-Cherng,Kuo, Sheng-Chu,Huang, Li-Jiau
, p. 785 - 790 (2008/03/12)
In our continuing search for potential anticancer candidates, 2-(3-methoxyphenyl)-6-pyrrolidinyl-4-quinazolinone (JJC-1) was selected as the lead compound. Starting 5-pyrrolidinyl-2-aminobenzamide was prepared using standard methodology from 5-chloro-2-ni
CONDENSED PYRIDINES AND PYRIMIDINES AND THEIR USE AS ALK-5 RECEPTOR LIGANDS
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Page 23, (2010/02/07)
Therapeutically active substituted quinoline and quinazoline compounds derivatives of formula (I) wherein X is N or CH, Y is NH, N (alkyl) or NH-CH2, and R2 and R3 are specified heterorings, the use thereof in therapy, particularly in the treatment or prophylaxis of disorders characterised by overexpression of transforming growth factor β (TGF-β), and pharmaceutical compositions for use in such therapy are disclosed.
2-phenyl-4-quinazolinone compounds, 2-phenyl-4-alkoxy-quinazoline compounds and their pharmaceutical compositions
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, (2008/06/13)
Two series of 6,7,2′,3′,4′,5′-substituted 2-phenyl-4-quinazolinones and 6,2′,3′,4′,5′-substituted 2,3-dihydro-2-phenyl-4-quinazolinones are synthesized and evaluated for cytotoxicity against a panel of human tumor cell lines, such as epidermoid carcinoma of the nasopharynx (KB), lung carcinoma (A-549), ileocecal carcinoma (HCT-8), breast cancer (MCF-7), melanoma (SKMEL-2), ovarian cancer (1A9), glioblastoma (U-87-MG), bone (HOS), P-gp-expressing epidermoid carcinoma of the nasopharynx (KB-VIN), and prostate cancer (PC3) cell lines, and some of the compounds are found potent. The present invention also synthesizes 2-phenyl-4-alkoxy-quinazoline compounds, wherein some of the compounds exhibit antiplatelet activity.
The Synthesis of Substituted 2-Aryl-4(3H)-Quinazolinones using NaHSO3/DMA. Steric Effect upon the Cyclisation-dehydrogenation Step
Lopez, Simon E.,Rosales, Monica E.,Urdaneta, Neudo,Godoy, M. Valentina,Charris, Jaime E.
, p. 716 - 726 (2007/10/03)
A number of 2-aryl substituted 6-pyrrolidino-4(3H)-quinazolinones are reported. They were synthesized in four steps starting from commercially available 5-chloro-2-nitrobenzoic acid. The key cyclisation-dehydrogenation step between 2-amino-pyrrolidinobenz
6-alkylamino- and 2,3-dihydro-3′-methoxy-2-phenyl-4-quinazolinones and related compounds: Their synthesis, cytotoxicity, and inhibition of tubulin polymerization
Hour,Huang,Kuo,Xia,Bastow,Nakanishi,Hamel,Lee
, p. 4479 - 4487 (2007/10/03)
As part of our continuing search for potential anticancer candidates among 2-phenyl-4-quinolones and 2-phenyl-4-quinazolinones, two series of 6,7,2′,3′,4′,5′-substituted 2-phenyl-4-quinazolinones and 6,2′,3′,4′,5′-substituted 2,3-dihydro-2-phenyl-4-quinazolinones were synthesized and evaluated for cytotoxicity and as inhibitors of tubulin polymerization. In general, a good correlation was found between the two activities. Five of the 6-substituted heterocyclic 2-phenyl-4-quinozolinones (37-51) showed significant cytotoxicity against a panel of human tumor cell lines with EC50 values in the low micromolar to nanomolar concentration ranges. Compound 38 was the most potent of these compounds, as well as the most potent inhibitor of tubulin polymerization in this series. The activity of 38 was in the same range as those of the antimitotic natural products, colchicine, podophyllotoxin, and combretastatin A-4. Substituted 2-phenyl-4-quinazolinones and 2,3-dihydro-2-phenyl-4-quinazolinones also displayed highly selective cytotoxicity against the ovarian cancer 1A9 and P-gp resistant KB-VIN cell lines.
