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, Biological Activity, and Molecular Dynamics Study of Novel Series of a Trimethoprim Analogs as Multi-Targeted Compounds: Dihydrofolate Reductase (DHFR) Inhibitors and DNA-Binding Agents.
TL;DR: In this paper, 18 trimethoprim analogs containing amide bonds were synthesized and compared with TMP, methotrexate (MTX), and netropsin (NT).
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Mo (CO)6‐assisted Pd‐supported magnetic graphene oxide‐catalyzed carbonylation‐cyclization as an efficient way for the synthesis of 4(3H)‐quinazolinones
Saeed Bahadorikhalili,Samira Ansari,Haleh Hamedifar,Leila Ma’mani,Mohsen Babaei,Rahim Eqra,Mohammad Mahdavi +6 more
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Ru(II)–arene complexes with N-substituted 3,4-dihydroquinazoline ligands and catalytic activity for transfer hydrogenation reaction
TL;DR: In this paper, N-coordinated 3,4-dihydroquinazoline ruthenium(II) complexes were synthesized by the cleavage reaction of [RuCl2(p-cymene)]2 with N-substituted 3, 4-dioxinazolines.
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Synthesis and screening of 2-(2-(4-substituted piperazine-1-yl)-5-phenylthiazol-4-yl)-3-aryl quinazolinone derivatives as anticancer agents
Ritesh N. Sharma,Rasik Ravani +1 more
TL;DR: Structural activity relationship of synthesized analogs suggested that the presence of NH linker with aryl moiety at the third position of quinazolinone ring was important for potent anticancer activity.
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.