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  • Lindgren, Anders E. G.Umeå universitet,Kemiska institutionen (author)

Chemical Probes to Study ADP-Ribosylation : Synthesis and Biochemical Evaluation of Inhibitors of the Human ADP-Ribosyltransferase ARTD3/PARP3

  • Article/chapterEnglish2013

Publisher, publication year, extent ...

  • 2013-11-22
  • American Chemical Society (ACS),2013
  • printrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:umu-84774
  • https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-84774URI
  • https://doi.org/10.1021/jm401394uDOI
  • http://kipublications.ki.se/Default.aspx?queryparsed=id:127955962URI

Supplementary language notes

  • Language:English
  • Summary in:English

Part of subdatabase

Classification

  • Subject category:ref swepub-contenttype
  • Subject category:art swepub-publicationtype

Notes

  • The racemic 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[1-(pyridin-2-yl)ethyl]propanamide, 1, has previously been identified as a potent but unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3). Herein we describe synthesis and evaluation of SS compounds in this class. It was found that the stereochemistry is of great importance for both selectivity and potency and that substituents on the phenyl ring resulted in poor solubility. Certain variations at the meso position were tolerated and caused a large shift in the binding pose. Changes to the ethylene linker that connects the quinazolinone to the amide were also investigated but proved detrimental to binding. By combination of synthetic organic chemistry and structure-based design, two selective inhibitors of ARTD3 were discovered.

Subject headings and genre

Added entries (persons, corporate bodies, meetings, titles ...)

  • Karlberg, TobiasKarolinska Institutet (author)
  • Ekblad, TorunKarolinska Institutet (author)
  • Spjut, SaraUmeå universitet,Kemiska institutionen(Swepub:umu)saaspt99 (author)
  • Thorsell, Ann-GerdKarolinska Institutet (author)
  • Andersson, C. DavidUmeå universitet,Kemiska institutionen(Swepub:umu)dadaon01 (author)
  • Nhan, Ton TongUmeå universitet,Kemiska institutionen (author)
  • Hellsten, VictorUmeå universitet,Kemiska institutionen (author)
  • Weigelt, Johan (author)
  • Linusson, AnnaUmeå universitet,Kemiska institutionen(Swepub:umu)analin99 (author)
  • Schuler, HerwigKarolinska Institutet (author)
  • Elofsson, MikaelUmeå universitet,Kemiska institutionen(Swepub:umu)miel0001 (author)
  • Umeå universitetKemiska institutionen (creator_code:org_t)

Related titles

  • In:Journal of Medicinal Chemistry: American Chemical Society (ACS)56:23, s. 9556-95680022-26231520-4804

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