Novel Pyridazin-3(2H)-one-Based Guanidine Derivatives as Potential DNA Minor Groove Binders with Anticancer Activity
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DOI: 10.1021/acsmedchemlett.1c00633
Abstract: Novel aryl guanidinium analogues containing the pyridazin-3(2H)-one core were proposed as minor groove binders (MGBs) with the support of molecular docking studies. The target dicationic or monocationic compounds, which show the guanidium group at different… read more here.
Keywords: one based; guanidine; pyridazin one; minor groove ... See more keywords
Disruption of nucleosomes by DNA groove binders of clinical significance and implications for chromatin remodeling.
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DOI: 10.1073/pnas.2216611120
Abstract: Small molecules that bind in the minor groove of DNA are in clinical use as antibiotics and antitumor drugs. Two members of this class of molecules, netropsin and chromomycin, are shown here to displace DNA… read more here.
Keywords: dna; disruption nucleosomes; nucleosomes dna; groove binders ... See more keywords
Evaluation of minor groove binders (MGBs) as novel anti-mycobacterial agents and the effect of using non-ionic surfactant vesicles as a delivery system to improve their efficacy
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Antimicrobial Chemotherapy"
DOI: 10.1093/jac/dkx326
Abstract: Objectives The slow development of major advances in drug discovery for the treatment of Mycobacterium tuberculosis (Mtb) infection suggests a compelling need for evaluation of more effective drug therapies against TB. New classes of drugs… read more here.
Keywords: anti mycobacterial; minor groove; evaluation; binders mgbs ... See more keywords
Four pyrrole derivatives used as building blocks in the synthesis of minor-groove binders
Sign Up to like & getrecommendations! Published in 2017 at "Acta Crystallographica Section E: Crystallographic Communications"
DOI: 10.1107/s2056989017001177
Abstract: The title nitropyrrole-based compounds are intermediates used in the synthesis of modified DNA minor-groove binders. They are ethyl 4-nitro-1H-pyrrole-2-carboxylate, its derivative ethyl 4-nitro-1-(4-pentynyl)-1H-pyrrole-2-carboxylate, N-[3-(dimethylamino)propyl]-1-isopentyl-4-nitro-1H-pyrrole-2-carboxamide and 1-(3-azidopropyl)-4-(1-methyl-4-nitro-1H-pyrrole-2-carboxamido)-N-[2-(morpholin-4-yl)ethyl]-1H-pyrrole-2-carboxamide. read more here.
Keywords: pyrrole; nitro pyrrole; minor groove; groove binders ... See more keywords
Synthesis and Evaluation of Novel DNA Minor Groove Binders as Antiamoebic Agents
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DOI: 10.3390/antibiotics11070935
Abstract: The free-living amoeba Acanthamoeba castellanii is responsible for the central nervous infection granulomatous amoebic encephalitis and sight-threatening infection Acanthamoeba keratitis. Moreover, no effective treatment is currently present, and a combination drug therapy is used. In… read more here.
Keywords: compounds mgb3; minor groove; groove binders; dna minor ... See more keywords
Selective Anti-Leishmanial Strathclyde Minor Groove Binders Using an N-Oxide Tail-Group Modification
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms231911912
Abstract: The neglected tropical disease leishmaniasis, caused by Leishmania spp., is becoming more problematic due to the emergence of drug-resistant strains. Therefore, new drugs to treat leishmaniasis, with novel mechanisms of action, are urgently required. Strathclyde… read more here.
Keywords: selective anti; minor groove; groove binders; strathclyde minor ... See more keywords