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  • Ayesa, SusanaStockholms universitet,Institutionen för organisk kemi (author)

Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S : Effect of sulfonamides P3 substituents on potency and selectivity.

  • Article/chapterEnglish2009

Publisher, publication year, extent ...

  • Elsevier,2009
  • printrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:su-35087
  • https://urn.kb.se/resolve?urn=urn:nbn:se:su:diva-35087URI
  • https://doi.org/10.1016/j.bmc.2008.12.020DOI

Supplementary language notes

  • Language:English
  • Summary in:English

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

Notes

  • Highly potent and selective 4-amidofuran-3-one inhibitors of cathepsin S are described. The synthesis and structure–activity relationship of a series of inhibitors with a sulfonamide moiety in the P3 position is presented. Several members of the series show sub-nanomolar inhibition of the target enzyme as well as an excellent selectivity profile and good cellular potency. Molecular modeling of the most interesting inhibitors describes interactions in the extended S3 pocket and explains the observed selectivity towards cathepsin K.

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

  • Lindquist, CharlottaStockholms universitet,Institutionen för organisk kemi,Bertil Samuelsson(Swepub:su)chli3135 (author)
  • Agback, Tatiana (author)
  • Benkestock, Kurt (author)
  • Classon, Björn (author)
  • Henderson, Ian (author)
  • Hewitt, Ellen (author)
  • Jansson, Katarina (author)
  • Kallin, Anders (author)
  • Sheppard, Dave (author)
  • Samuelsson, Bertil (author)
  • Stockholms universitetInstitutionen för organisk kemi (creator_code:org_t)

Related titles

  • In:Bioorganic & Medicinal Chemistry: Elsevier17:3, s. 1307-13240968-08961464-3391

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