About: Synthesis of distal and proximal fleximer base analogues and evaluation in the nucleocapsid protein of HIV-1

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About: Synthesis of distal and proximal fleximer base analogues and evaluation in the nucleocapsid protein of HIV-1 Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

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type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Synthesis of distal and proximal fleximer base analogues and evaluation in the nucleocapsid protein of HIV-1
Creator	Seley-Radtke, Katherine Heng, Xiao Botta, Maurizio Marchant, Jan Ku, Therese Lopresti, Natalie Mori, Mattia Shirley, Matthew Summers, Michael
Source	Elsevier; Medline; PMC
abstract	Anti-HIV-1 drug design has been notably challenging due to the virus’ ability to mutate and develop immunity against commercially available drugs. The aims of this project were to develop a series of fleximer base analogues that not only possess inherent flexibility that can remain active when faced with binding site mutations, but also target a non-canonical, highly conserved target: the nucleocapsid protein of HIV (NC). The compounds were predicted by computational studies not to function via zinc ejection, which would endow them with significant advantages over non-specific and thus toxic zinc-ejectors. The target fleximer bases were synthesized using palladium-catalyzed cross-coupling techniques and subsequently tested against NC and HIV-1. The results of those studies are described herein.
has issue date	2019-07-01(xsd:dateTime)
bibo:doi	10.1016/j.bmc.2019.05.019
bibo:pmid	31126822
has license	no-cc
sha1sum (hex)	2a0a1bbb35b07b464af24878a2013b61b2bf301d
schema:url	https://doi.org/10.1016/j.bmc.2019.05.019
resource representing a document's title	Synthesis of distal and proximal fleximer base analogues and evaluation in the nucleocapsid protein of HIV-1
has PubMed Central identifier	PMC6556414
has PubMed identifier	31126822
schema:publication	Bioorg Med Chem
resource representing a document's body	covid:2a0a1bbb35b07b464af24878a2013b61b2bf301d#body_text
is schema:about of	named entity 'compounds' named entity 'remain' named entity 'commercially' named entity 'mutate' named entity 'develop' named entity 'evaluation' named entity 'distal' named entity 'CONSERVED' named entity 'CROSS-COUPLING' named entity 'COMPUTATIONAL' named entity 'HIV' named entity 'highly' named entity 'zinc' named entity 'ejection' named entity 'nucleocapsid' named entity 'non-specific' named entity 'highly conserved' named entity 'NMR' named entity 'guanine' named entity 'organozinc' named entity 'NMR' named entity 'mmol' named entity 'column chromatography' named entity 'mmol' named entity 'methyl' named entity 'moiety' named entity 'electron' named entity 'Bruker' named entity 'AVANCE' named entity 'TMSCl' named entity 'mmol' named entity 'silica gel' named entity 'HIV-1' named entity 'room temperature' named entity 'mmol' named entity 'guanine' named entity 'EDTA' named entity 'silica gel' named entity 'RNA' named entity 'mmol' named entity 'glycerol' named entity 'EtOAc' named entity 'deprotected' named entity 'room temperature' named entity 'room temperature' named entity 'OpenEye' named entity 'Lithium halogen exchange' named entity 'HIV-1' named entity 'spectroscopically' named entity 'starting material' named entity 'w/v' named entity 'EtOAc' named entity 'H NMR' named entity 'THF' named entity 'mmol' named entity 'gradient' named entity 'acetic acid' named entity 'encapsidation' named entity 'distal' named entity 'distal' named entity 'mmol' named entity 'mmol' named entity 'iodo' named entity 'interact' named entity 'silica gel' named entity 'pepstatin' named entity 'acetic anhydride' named entity 'aromatic' named entity 'silica gel' named entity 'protein' named entity 'column chromatography' named entity 'TLC' named entity 'mmol'

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