Structure-activity relationship of indoline-2-carboxylic acid N-(substituted)phenylamide derivatives

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4620-3. doi: 10.1016/j.bmcl.2010.06.004. Epub 2010 Jun 8.

Abstract

Chroman derivatives exhibited potent inhibitory activity of NF-kappaB. For SAR, the chroman scaffold was modified with an indoline moiety. A series of indoline-2-carboxylic acid N-(substituted)phenylamide derivatives were synthesized to explore their inhibitory activities of NF-kappaB and they were also evaluated for cytotoxicity against various cancer cell lines. Since intermediates with Boc showed outstanding results, various substituents in place of the Boc group were introduced additionally and these compounds were also evaluated for SAR.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / toxicity
  • Benzylamines / chemical synthesis
  • Benzylamines / chemistry*
  • Benzylamines / toxicity
  • Cell Line, Tumor
  • Chromans / chemistry
  • Drug Screening Assays, Antitumor
  • Humans
  • Indoles / chemistry*
  • NF-kappa B / antagonists & inhibitors
  • NF-kappa B / metabolism
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Benzylamines
  • Chromans
  • Indoles
  • NF-kappa B
  • indoline
  • benzylamine