Literature DB >> 15876538

Studies on quinones. Part 39: Synthesis and leishmanicidal activity of acylchloroquinones and hydroquinones.

Jaime A Valderrama1, Carlos Zamorano, M Florencia González, Eric Prina, Alain Fournet.   

Abstract

Acylhydroquinone-based compounds are attractive targets for the design of new leishmanicidal drugs. We have previously described sesquiterpene quinones and hydroquinones series, which exhibit different degree of potency against Leishmania amazonensis. The present study details the preparation of acylchloroquinones and hydroquinones possessing lipophilic substituents and examines their in vitro activity against intracellular L. amazonensis amastigotes. The quinone or hydroquinone nucleus is essential for the activity of the members of the series. The lipophilicity of the cycloaliphatic systems in these members seems to attenuate the cytotoxical effect and increases the selectivity of those compounds containing the norbornene system.

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Year:  2005        PMID: 15876538     DOI: 10.1016/j.bmc.2005.04.041

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  3 in total

1.  Design, synthesis and biological evaluation of fused naphthofuro[3,2-c] quinoline-6,7,12-triones and pyrano[3,2-c]quinoline-6,7,8,13-tetraones derivatives as ERK inhibitors with efficacy in BRAF-mutant melanoma.

Authors:  Ashraf A Aly; Essmat M El-Sheref; Momtaz E M Bakheet; Mai A E Mourad; Stefan Bräse; Mahmoud A A Ibrahim; Martin Nieger; Boyan K Garvalov; Kevin N Dalby; Tamer S Kaoud
Journal:  Bioorg Chem       Date:  2018-10-23       Impact factor: 5.275

2.  In Silico Antiprotozoal Evaluation of 1,4-Naphthoquinone Derivatives against Chagas and Leishmaniasis Diseases Using QSAR, Molecular Docking, and ADME Approaches.

Authors:  Lina S Prieto Cárdenas; Karen A Arias Soler; Diana L Nossa González; Wilson E Rozo Núñez; Agobardo Cárdenas-Chaparro; Pablo R Duchowicz; Jovanny A Gómez Castaño
Journal:  Pharmaceuticals (Basel)       Date:  2022-05-31

3.  Access to New Cytotoxic Quinone-Amino Acid Conjugates Linked through A Vinylic Spacer from 2-Acylnaphthoquinones and Methyl 3-Aminocrotonate.

Authors:  Jaime A Valderrama; Joel Garrido; Virginia Delgado; Julio Benites; Cristina Theoduloz
Journal:  Molecules       Date:  2017-12-20       Impact factor: 4.411

  3 in total

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