Journal ArticleDOI
Antiviral agents 2. Synthesis of trimeric naphthoquinone analogues of conocurvone and their antiviral evaluation against HIV.
Ian Travers Crosby,David Gerard Bourke,Eric Dale Jones,Paula J De Bruyn,David Rhodes,Nick Vandegraaff,Susan Cox,Jonathan Coates,Alan D. Robertson +8 more
TLDR
A maleimide derivative, where the central quinone between the pendant hydroxyquinones was replaced, was successfully synthesised and although it exhibited comparable enzyme inhibitory activity it had negligible HIV inhibitory cellular activity.About:
This article is published in Bioorganic & Medicinal Chemistry.The article was published on 2010-09-01. It has received 21 citations till now. The article focuses on the topics: Naphthoquinone & Pyran.read more
Citations
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Chiral Squaramide-Catalyzed Highly Enantioselective Michael Addition of 2-Hydroxy-1,4-naphthoquinones to Nitroalkenes
Wen Yang,Da-Ming Du +1 more
TL;DR: A chiral squaramide-organocatalyzed, highly enantioselective Michael addition of 2-hydroxy-1,4-naphthoquinones to nitroalkenes has been developed and provides an efficient alternative route toward the synthesis of chiral functionalized naphthOquinones.
Journal ArticleDOI
Catalytic asymmetric reactions and synthesis of quinones
Basavaprabhu Hosamani,Matheus F. Ribeiro,Eufrânio N. da Silva Júnior,Irishi N. N. Namboothiri +3 more
TL;DR: Asymmetric reactions and the synthesis of various quinones, carried out in the presence of chiral organocatalysts and metal-ligand complexes, are reviewed here.
Journal ArticleDOI
Towards targeting anticancer drugs: ruthenium(ii)-arene complexes with biologically active naphthoquinone-derived ligand systems.
Mario Kubanik,Wolfgang Kandioller,Kunwoo Kim,Robert F. Anderson,Erik Klapproth,Michael A. Jakupec,Alexander Roller,Tilo Söhnel,Bernhard K. Keppler,Christian G. Hartinger,Christian G. Hartinger +10 more
TL;DR: The preparation of 2-hydroxy-[1,4]-naphthoquinone-derived ligands and their coordination to a Ru(II)(η(6)-p-cymene)Cl moiety resulted in the surprising formation of nitroso-naphthalene complexes, as confirmed by X-ray diffraction analysis.
Journal ArticleDOI
Design concepts of half-sandwich organoruthenium anticancer agents based on bidentate bioactive ligands
William D.J. Tremlett,David M. Goodman,Tasha R. Steel,Saawan Kumar,Anna Wieczorek-Błauż,Fearghal P. Walsh,Matthew P. Sullivan,Muhammad Hanif,Christian G. Hartinger +8 more
TL;DR: Five design concepts are identified and explored and their application to half-sandwich organoruthenium anticancer compounds in which the bioactive ligand is coordinated to the Ru center through a bidentate chelating motif are explored.
Journal ArticleDOI
Antibacterial naphthoquinone derivatives targeting resistant strain Gram-negative bacteria in biofilms.
Juliana S. Novais,Caroline S. Moreira,Ana Carolina J. A. Silva,Raquel de S. Loureiro,Agnes Marie Sá Figueiredo,Vitor F. Ferreira,Helena Carla Castro,David R. da Rocha +7 more
TL;DR: 12 new naphthoquinones with antimicrobial activity against Gram-negative and Gram-positive strains and biofilm inhibition data showed compounds, 9e, 9f, 9j and 9k, are anti-biofilm molecules when used in sub-MIC concentrations against P. aeruginosa ATCC 15442 strain.
References
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Retroviral intasome assembly and inhibition of DNA strand transfer
Stephen Hare,Saumya Shree Gupta,Saumya Shree Gupta,Eugene Valkov,Eugene Valkov,Alan Engelman,Peter Cherepanov +6 more
TL;DR: The crystal structure of full-length integrase from the prototype foamy virus in complex with its cognate DNA is presented, defining the structural basis of retroviral DNA integration, and will allow modelling of the HIV-1 intasome to aid in the development of antiretroviral drugs.
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The impact of natural products upon modern drug discovery
TL;DR: This work analyzes natural product leads in the Lipinski and parallel universe in terms of drug-like properties, and shows that they can be divided into two equal subsets that complies with the Rule of Five.
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Lewis Acid and Hexamethyldisilazane-Promoted Efficient Synthesis of N-Alkyl- and N-Arylimide Derivatives.
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Strand transfer inhibitors of HIV-1 integrase: bringing IN a new era of antiretroviral therapy.
Damian J. McColl,Xiaowu Chen +1 more
TL;DR: One INSTI, raltegravir (RAL), was approved in late 2007 for the treatment of HIV-1 infection in patients with prior antiretroviral (ARV) treatment experience and was recently approved also for first line therapy.
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The history of antiretrovirals: key discoveries over the past 25 years.
TL;DR: These compounds are used in various drug combination regimens so as to achieve the highest possible benefit and tolerability, and to diminish the risk of virus-drug resistance development.