ArticleJournal of medicinal chemistry2012
Searching for new chemotherapies for tropical diseases: ruthenium-clotrimazole complexes display high in vitro activity against Leishmania major and Trypanosoma cruzi and low toxicity toward normal mammalian cells.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 119 citations in OpenAlex.
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- Resurgence and Repurposing of Antifungal Azoles by Transition Metal Coordination for Drug Discovery.Pharmaceutics · 2023Review
- Half-Sandwich Type Platinum-Group Metal Complexes ofMolecules (Basel, Switzerland) · 2023Article
- Computer-Aided Drug Design and Synthesis of Rhenium Clotrimazole Antimicrobial Agents.Antibiotics (Basel, Switzerland) · 2023Article
- Half-Sandwich Rhodium Complexes with Releasable N-Donor Monodentate Ligands: Solution Chemical Properties and the Possibility for Acidosis Activation.Pharmaceutics · 2023Article
- Redesigning Nature: Ruthenium Flavonoid Complexes with Antitumour, Antimicrobial and Cardioprotective Activities.Molecules (Basel, Switzerland) · 2021Review
- Ruthenium Complexes in the Fight against Pathogenic Microorganisms. An Extensive Review.Pharmaceutics · 2021Review
- Enhancing the Activity of Drugs by Conjugation to Organometallic Fragments.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Review
- Development of Thiophene Compounds as Potent Chemotherapies for the Treatment of Cutaneous Leishmaniasis Caused byMolecules (Basel, Switzerland) · 2018Article
- Characterization of the Activities of Dinuclear Thiolato-Bridged Arene Ruthenium Complexes against Toxoplasma gondii.Antimicrobial agents and chemotherapy · 2017Article
- Ruthenium-Clotrimazole complex has significant efficacy in the murine model of cutaneous leishmaniasis.Acta tropica · 2016Article
- A novel class of piperidones exhibit potent, selective and pro-apoptotic anti-leukemia properties.Oncology letters · 2016Article
- Antiplasmodial activity of iron(II) and ruthenium(II) organometallic complexes against Plasmodium falciparum blood parasites.Memorias do Instituto Oswaldo Cruz · 2015Article
- Novel arylalkylamine compounds exhibits potent selective antiparasitic activity against Leishmania major.Bioorganic & medicinal chemistry letters · 2015Article
- Evaluation of α,β-unsaturated ketones as antileishmanial agents.Antimicrobial agents and chemotherapy · 2015Article
- Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis.Chemical reviews · 2014Review
- Nitro/nitrosyl-ruthenium complexes are potent and selective anti-Trypanosoma cruzi agents causing autophagy and necrotic parasite death.Antimicrobial agents and chemotherapy · 2014Article
- Analysis of the cytotoxic effects of ruthenium-ketoconazole and ruthenium-clotrimazole complexes on cancer cells.Cell biology and toxicology · 2013Article
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Authors and funding
10 authors at 5 institutions in 2 countries.
Funding
Abstract
Eight new ruthenium complexes of clotrimazole (CTZ) with high antiparasitic activity have been synthesized, cis,fac-[Ru(II)Cl(2)(DMSO)(3)(CTZ)] (1), cis,cis,trans-[Ru(II)Cl(2)(DMSO)(2)(CTZ)(2)] (2), Na[Ru(III)Cl(4)(DMSO)(CTZ)] (3), Na[trans-Ru(III)Cl(4)(CTZ)(2)] (4), [Ru(II)(η(6)-p-cymene)Cl(2)(CTZ)] (5), [Ru(II)(η(6)-p-cymene)(bipy)(CTZ)][BF(4)](2) (6), [Ru(II)(η(6)-p-cymene)(en)(CTZ)][BF(4)](2) (7), and [Ru(II)(η(6)-p-cymene)(acac)(CTZ)][BF(4)] (8) (bipy = bipyridine; en = ethlylenediamine; acac = acetylacetonate). The crystal structures of compounds 4-8 are described. Complexes 1-8 are active against promastigotes of Leishmania major and epimastigotes of Trypanosoma cruzi. Most notably, complex 5 increases the activity of CTZ by factors of 110 and 58 against L. major and T. cruzi, with no appreciable toxicity to human osteoblasts, resulting in nanomolar and low micromolar lethal doses and therapeutic indexes of 500 and 75, respectively. In a high-content imaging assay on L. major-infected intraperitoneal mice macrophages, complex 5 showed significant inhibition on the proliferation of intracellular amastigotes (IC(70) = 29 nM), while complex 8 displayed some effect at a higher concentration (IC(40) = 1 μM).
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.