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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Bi(TFA)3–[nbp]FeCl4: a new, efficient and reusable promoter system for the synthesis of 4(3H)-quinazolinone derivatives
TL;DR: In this paper, a one-pot condensation of anthranilic acid, trimethyl orthoformate and primary amines in the presence of 5mmol% of Bi(TFA) 3 immobilized on [nbp]FeCl 4 as a room temperature ionic liquid is described.
Journal ArticleDOI
An efficient, one-pot, synthesis of dithiocarbamates from the corresponding alcohols using Mitsunobu’s reagent
Devdutt Chaturvedi,Suprabhat Ray +1 more
TL;DR: A novel Mitsunobu-based protocol was developed for the synthesis of carbamates from the corresponding alcohols using carbon dioxide and amines in good to excellent yields and is mild, chemoselective, and efficient compared to other reported methods.
Journal ArticleDOI
A highly efficient synthesis of dithiocarbamates in green reaction media
Najmadin Azizi,Elham Gholibeglo +1 more
TL;DR: In this article, a one-pot, three-component condensation of an amine, carbon disulfide, and a variety of electrophilic reagents in high yields and short reaction times without organic solvents and tedious work-up is described.
Journal ArticleDOI
Design, synthesis and antitumor evaluation of novel thalidomide dithiocarbamate and dithioate analogs against Ehrlich ascites carcinoma-induced solid tumor in Swiss albino mice
TL;DR: A series of 16 novel thalidomide sulfur analogs containing one and two sulfur atoms 2 and 4-18, respectively, were designed and synthesized as mentioned in this paper, and they were screened for in vitro antitumor activity against Ehrlich ascites carcinoma (EAC) cell line and exhibited potent cytotoxic activity.
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Acceptorless dehydrogenative condensation of o-aminobenzamides with aldehydes to quinazolinones in water catalyzed by a water-soluble iridium complex [Cp*Ir(H2O)3][OTf]2
TL;DR: In this paper, a general and efficient method for the synthesis of quinazolinones via acceptorless dehydrogenative condensation of o-aminobenzamides with aldehydes in water has been accomplished.
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.
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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.
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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.