ArticleBioorganic & medicinal chemistry2011
Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents.
Article in Bioorganic & medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers, 1 of them a synthesis that pooled it.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
11 citing papers in PubMed, 1 synthesis or guideline pooled it, 27 citations in OpenAlex.
- Novel amidines and analogues as promising agents against intracellular parasites: a systematic review.Parasitology · 2013Pooled it
- Synthesis, anticancer activity, docking and computational studies of new pyridyl-glycosyl hybrids and acyclic analogs.Future medicinal chemistry · 2024Article
- Repurposing Drugs to Fight Hepatic Malaria Parasites.Molecules (Basel, Switzerland) · 2020Review
- Indole and Benzimidazole Bichalcophenes: Synthesis, DNA Binding and Antiparasitic Activity.European journal of medicinal chemistry · 2018Article
- An overview of recent advances in duplex DNA recognition by small molecules.Beilstein journal of organic chemistry · 2018Review
- The unusual monomer recognition of guanine-containing mixed sequence DNA by a dithiophene heterocyclic diamidine.Biochemistry · 2014Article
- Evaluation of the biological activity of novel monocationic fluoroaryl-2,2'-bichalcophenes and their analogues.Drug design, development and therapy · 2014Article
- Anticancer, antioxidant activities, and DNA affinity of novel monocationic bithiophenes and analogues.Drug design, development and therapy · 2014Article
- Targeting the DNA-binding activity of the human ERG transcription factor using new heterocyclic dithiophene diamidines.Nucleic acids research · 2013Article
- Novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs as antibacterial agents: a structural activity relationship.Drug design, development and therapy · 2013Article
- Heterocyclic dications as a new class of telomeric G-quadruplex targeting agents.Current pharmaceutical design · 2012Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 4 institutions in 3 countries.
Funding
Abstract
A series of phenyl-2,2'-bichalcophene diamidines 1a-h were synthesized from the corresponding dinitriles either via a direct reaction with LiN(TMS)₂, followed by deprotection with ethanolic HCl or through the bis-O-acetoxyamidoxime followed by hydrogenation in acetic acid and EtOH over Pd-C. These diamidines show a wide range of DNA affinities as judged from their ΔT(m) values which are remarkably sensitive to replacement of a furan unit with a thiophene one. These differences are explained in terms of the effect of subtle changes in geometry of the diamidines on binding efficacy. Five of the eight compounds were highly active (below 6 nM IC₅₀) in vitro against Trypanosoma brucei rhodesiense (T. b. r.) and four gave IC₅₀values less than 7 nM against Plasmodium falciparum (P. f.). Only one of the compounds was as effective as reference compounds in the T. b. r. mouse model for the acute phase of African trypanosomiasis.
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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.