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Abstract

Structure-activity relationship studies of diaryl amine-type KSP inhibitors were carried out. Diaryl amine derivatives with a pyridine ring or urea group were less active when compared with the parent carboline and carbazole derivatives. Optimization studies of a lactam-fused diphenylamine-type KSP inhibitor revealed that the aniline NH group and 3-CF3 phenyl group were indispensable for potent KSP inhibition. Modification with a seven-membered lactam-fused phenyl group and a 4-(trifluoromethyl)pyridin-2-yl group improved aqueous solubility while maintaining potent KSP inhibitory activity. From these studies, we identified novel diaryl amine-type KSP inhibitors with a favorable balance of potency and solubility.

Journal

  • Bioorganic & medicinal chemistry

    Bioorganic & medicinal chemistry 22(12), 3171-3179, 2014-06-15

    Elsevier Ltd.

Codes

  • NII Article ID (NAID)
    120005466732
  • NII NACSIS-CAT ID (NCID)
    AA10938083
  • Text Lang
    ENG
  • Article Type
    journal article
  • ISSN
    0968-0896
  • Data Source
    IR 
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