Journal ArticleDOI
Synthesis and in vitro antitumor activity of 4(3H)-quinazolinone derivatives with dithiocarbamate side chains
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TLDR
A series of 4(3H)-quinazolinone derivatives with dithiocarbamate side chains were synthesized and tested for their in vitro antitumor activity against human myelogenous leukemia K562 cells, and Piperazine-1-carbodithioate 8q exhibited significant inhibitory activity.About:
This article is published in Bioorganic & Medicinal Chemistry Letters.The article was published on 2005-04-01. It has received 325 citations till now. The article focuses on the topics: Dithiocarbamate & Quinazolinone.read more
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Synthesis, characterization and evaluation of in vitro antioxidant and anti-inflammatory activity of 2-(4-oxo-2-phenylquinazolin-3(4H)-yl) substituted acetic acids
TL;DR: These two vital moieties were combined together into a single molecule by varying the different amino acids and synthesized, characterized and evaluated for anti-inflammatory and antimicrobial activities.
Journal ArticleDOI
DDQ in mechanochemical C–N coupling reactions
TL;DR: 2,3-Dichloro-5,6-dicyano-1,4-benzoquinone can be used to synthesize 1,2-disubstituted benzimidazoles and quinazolin-4(3H)-ones via the intra- and intermolecular C–N coupling reaction under solvent-free mechanochemical (ball milling) conditions.
Journal ArticleDOI
BF3.OEt2 Catalyzed Synthesis of Functionalized 9-fluorene-9-ylidene Appended Quinazolin-4-ones
TL;DR: An efficient method for the construction of the quinazolinone skeleton from the reaction of 9-(phenylethynyl)-9H-fluoren-9-ols with substituted 2-aminobenzamides catalyzed by boron trifluoride is achieved in this article .
Journal ArticleDOI
Well-defined manganese complex catalyzed dehydrogenative synthesis of quinazolin-4(3<i>H</i>)-ones and 3,4-dihydro-2<i>H</i>-1,2,4-benzothiadiazine 1,1-dioxides
TL;DR: The synthesis of N-heterocycles has been considered an emerging topic of chemical research due to its widespread usage in medicinal chemistry, materials science, and natural product synthesis as mentioned in this paper .
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Electro-oxidative cyclization: access to quinazolinones via K2S2O8 without transition metal catalyst and base
TL;DR: In this article, a K2S2O8-promoted oxidative tandem cyclization of primary alcohols with 2-aminobenzamides was successfully achieved under undivided electrolytic conditions without a transition metal and base.
References
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Cancer Chemopreventive Potential of Sulforamate, a Novel Analogue of Sulforaphane That Induces Phase 2 Drug-metabolizing Enzymes
Clarissa Gerhäuser,Min You,Jinfang Liu,Robert M. Moriarty,Michael E. Hawthorne,Rajendra G. Mehta,Richard C. Moon,John M. Pezzuto +7 more
TL;DR: The synthesis and activity of a novel cancer chemopreventive agent is reported, (+/-)-4-methylsulfinyl-1-(S-methyldithiocarbamyl)-butane (trivial name, sulforamate), an aliphatic analogue of brassinin with structural similarities to sulforaphane, which can be regarded as a readily available promising new cancer chemobiotic responsive agent.
Journal ArticleDOI
Cancer chemopreventive activity of brassinin, a phytoalexin from cabbage
Rajendra G. Mehta,Jinfang Liu,Andreas I. Constantinou,Cathy F. Thomas,Michael E. Hawthorne,Min You,Clarissa Gerhäuser,John M. Pezzuto,Richard C. Moon,Robert M. Moriarty +9 more
TL;DR: Brassinin may be effective as a chemopreventive agent during both the initiation and promotion phases of carcinogenesis, and the synthetic route described herein has proven amenable for scale-up production.
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Pemetrexed disodium, a novel antifolate with multiple targets
Nicola J. Curtin,AN Hughes +1 more
TL;DR: Preclinical studies indicate that the toxic effects of pemetrexed can be reduced by dietary folate, resulting in an improved therapeutic index and low folate status is also associated with higher levels of toxicity in patients.
Journal ArticleDOI
Quinazoline antifolate thymidylate synthase inhibitors: heterocyclic benzoyl ring modifications.
Marsham Pr,Leslie Richard Hughes,Ann L. Jackman,A. J. Hayter,J. Oldfield,Wardleworth Jm,J. A. M. Bishop,O'Connor Bm,Alan Hilary Calvert +8 more
TL;DR: The enhanced cytotoxicities of the thiophene and thiazole analogues result, at least in part, from their efficient transport into the cells via the reduced folate carrier mechanism and very good substrate activity for folylpolyglutamate synthetase.
Journal ArticleDOI
AG337, a novel lipophilic thymidylate synthase inhibitor: in vitro and in vivo preclinical studies.
Stephanie Webber,Charlotte A. Bartlett,Theodore Boritzki,Jill A. Hilliard,Eleanor F. Howland,Amanda L. Johnston,Maha Kosa,Stephen Margosiak,C. A. Morse,Bhasker V. Shetty +9 more
TL;DR: In vivo, AG337 was highly active against the thymidine kinase-deficient murine L5178Y/TK- lymphoma implanted either i.p.m. or oral delivery, suggesting, as would be expected for a lipophilic agent, that there is rapid influx and efflux from cells and no intracellular metabolism to derivatives with enhanced retention.