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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Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines.
TL;DR: SAR studies revealed that the substituents on C6 and C7 positions of quinazoline, the amine component of dithiocarbamate moiety and the linker greatly affected the activity of the EGFR inhibitors, providing a promising new strategy for the preparation of potent tyrosine kinase inhibitors.
Journal ArticleDOI
Synthesis, characterization and antifungal activities of 3d-transition metal complexes of 1-acetylpiperazinyldithioc arbamate, M(acpdtc) 2
TL;DR: The thermogravimetric and differential scanning calorimetric profile of the ligand indicates a two-step decomposition pattern while the complexes exhibit a three-stage thermogram forming metal sulfide as the eventual end product.
Journal ArticleDOI
Synthesis and anticancer activity of N-substituted 2-arylquinazolinones bearing trans-stilbene scaffold
Mohammad Mahdavi,Keyvan Pedrood,Maliheh Safavi,Mina Saeedi,Mahboobeh Pordeli,Sussan Kabudanian Ardestani,Saeed Emami,Mehdi Adib,Alireza Foroumadi,Abbas Shafiee +9 more
TL;DR: The morphological analysis by acridine orange/ethidium bromide double staining test and flow cytometry analysis indicated that the prototype compound 7h can induce apoptosis in MCF-7 and MDA-MB-231 cells.
Journal ArticleDOI
Rapid assembly of quinazolinone scaffold via copper-catalyzed tandem reaction of 2-bromobenzamides with aldehydes and aqueous ammonia: application to the synthesis of the alkaloid tryptanthrin
TL;DR: In this paper, a copper-catalyzed tandem reaction of 2-bromobenzamides with aldehydes and aqueous ammonia under air was demonstrated for the synthesis of tryptanthrin.
Journal ArticleDOI
Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates
Yan Zou,Shichong Yu,Renwu Li,Qingjie Zhao,Xiang Li,Mao-cheng Wu,Ting Huang,Xiaoxun Chai,Honggang Hu,Qiuye Wu +9 more
TL;DR: In vitro biological activities of 2b, 3a, 3c, 3h-k, and 3o-q against Candida species were much better than those of fluconazole and ketoconazole, and Computational docking experiments indicated that the inhibition of CYP51 involved a coordination bond with iron of the heme group, the hydrophilic H-bonding region, the Hydrophobic region, and the narrow hydrophobic cleft.
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.
Journal ArticleDOI
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.