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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Simple and scalable electrosynthesis of 1H-1-hydroxy-quinazolin-4-ones
Olesja Koleda,Tobias Prenzel,Johannes G. Winter,Tomoki Hirohata,María de Jesús Gálvez-Vázquez,Dieter Schollmeyer,Shinsuke Inagi,Edgars Suna,Siegfried R. Waldvogel +8 more
TL;DR: In this article , a carbon-based electrode material and constant current conditions are used for cathodic synthesis of 1-hydroxy- and 1-oxy-quinazolin-4-ones from easily accessible nitro starting materials.
Journal ArticleDOI
Arsenic(III) mixed derivatives having oximes and morpholinedithiocarbamate along with their cytotoxic, antimicrobial, and antioxidant studies.
TL;DR: These derivatives examined against microbes and results revealed that these derivatives expressed more antifungal potential than antibacterial in comparison with conventional arsenic(III)chloride.
Journal ArticleDOI
Solar-Driven Thermocatalytic Synthesis of Octahydroquinazolinone Using Novel Polyvinylchloride (PVC)-Supported Aluminum Oxide (Al2O3) Catalysts
Abdulrahman I. Alharthi,Mshari A. Alotaibi,Amani M. Alansi,Talal F. Qahtan,Imtiaz Ali,Md. Afroz Bakht +5 more
TL;DR: In this paper , a solar-driven thermocatalytic synthesis of octahydroquinazolinone using polyvinylchloride (PVC)-supported aluminum oxide (Al2O3) as a catalyst under natural sunlight is proposed.
Journal ArticleDOI
Synthesis and Analgesic Activity of 5,6-difluoro-2-Methyl-4H-benzo(d) (1,3)-Oxazin-4-one and 3-Amino-5,6-difluoro-2-Mehtyl-quinzolin 4(3H)-One
TL;DR: The synthesized compounds 1and 2 showed significant activity as an Anagesic agent and screened against various strains of microorganism, Staphylococcus aureus, Bacillus species, Escherichia coli, Klebsiella pneumonia, Serratia Marcensces, and Candida albicans.
Action of Nitrogen and Carbon Nucleophiles on Benzoxazin-4(H)-one Derivative as Convenient Methods for the Synthesis of Some Novel Heterocyclic Systems
A. I. Salem,Mohammad E. Azab +1 more
TL;DR: In this paper, N-substituted quinazolin-4(H)-one, 1-H-pyridazino[6,1b]-, [1,2]oxazino-[3,2-b], benzimidazolo[1, 2-c]quinazoline, [ 1,2,4]-triazolo [2,3-c], [1.3,4]quinazoline derivatives, [3,1]triazoles derivatives were obtained via the reaction of 2-[
References
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Journal Article
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.