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  • Carbajales, Carlos (author)

Structure-Based Design of New KSP-Eg5 Inhibitors Assisted by a Targeted Multicomponent Reaction

  • Article/chapterEnglish2014

Publisher, publication year, extent ...

  • 2014-06-18
  • Wiley,2014
  • printrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:uu-229714
  • https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-229714URI
  • https://doi.org/10.1002/cbic.201402089DOI

Supplementary language notes

  • Language:English
  • Summary in:English

Part of subdatabase

Classification

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

Notes

  • An integrated multidisciplinary approach that combined structure-based drug design, multicomponent reaction synthetic approaches and functional characterization in enzymatic and cell assays led to the discovery of new kinesin spindle protein (KSP) inhibitors with antiproliferative activity. A focused library of new benzimidazoles obtained by a Ugi + Boc removal/cyclization reaction sequence generated low-micromolar-range KSP inhibitors as promising anticancer prototypes. The design and functional studies of the new chemotypes were assessed by computational modeling and molecular biology techniques. The most active compounds-20 (IC50=1.49 mu m, EC50=3.63 mu m) and 22 (IC50=1.37 mu m, EC50=6.90 mu m)-were synthesized with high efficiency by taking advantage of the multicomponent reactions.

Subject headings and genre

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

  • Prado, Miguel Angel (author)
  • Gutierrez-de-Teran, HugoUppsala universitet,Beräknings- och systembiologi(Swepub:uu)hugut367 (author)
  • Cores, Angel (author)
  • Azuaje, Jhonny (author)
  • Novio, Silvia (author)
  • Jesus Nunez, Maria (author)
  • Fernandez-Garcia, Belen (author)
  • Sotelo, Eddy (author)
  • Garcia-Mera, Xerardo (author)
  • Sanchez-Lazo, Pedro (author)
  • Freire-Garabal, Manuel (author)
  • Coelho, Alberto (author)
  • Uppsala universitetBeräknings- och systembiologi (creator_code:org_t)

Related titles

  • In:ChemBioChem: Wiley15:10, s. 1471-14801439-42271439-7633

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