Novel substituted (Z)-5-((N-benzyl-1H-indol-3-yl)methylene)imidazolidine-2,4-diones and 5-((N-benzyl-1H-indol-3-yl)methylene)pyrimidine-2,4,6(1H,3H,5H)-triones as potent radio-sensitizing agents

Bioorg Med Chem Lett. 2010 Jan 15;20(2):600-2. doi: 10.1016/j.bmcl.2009.11.082. Epub 2009 Nov 22.

Abstract

A series of (Z)-5-((N-benzyl-1H-indol-3-yl)methylene)imidazolidine-2,4-dione (9a-9m) and 5-((N-benzyl-1H-indol-3-yl)methylene)pyrimidine-2,4,6(1H,3H,5H)-trione (10a-10i) derivatives that incorporate a variety of aromatic substituents in both the indole and N-benzyl moieties have been synthesized. These analogs were evaluated for their radiosensitization activity against the HT-29 cell line. Three analogs, 10a, 10b, and 10c were identified as the most potent radiosensitizing agents.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / toxicity
  • Barbiturates / chemical synthesis
  • Barbiturates / chemistry*
  • Barbiturates / toxicity
  • Benzene / chemistry
  • HT29 Cells
  • Humans
  • Indoles / chemical synthesis
  • Indoles / chemistry*
  • Indoles / toxicity
  • Pyrimidines / chemical synthesis
  • Pyrimidines / chemistry*
  • Pyrimidines / toxicity
  • Radiation-Sensitizing Agents / chemical synthesis
  • Radiation-Sensitizing Agents / chemistry*
  • Radiation-Sensitizing Agents / toxicity

Substances

  • Antineoplastic Agents
  • Barbiturates
  • Indoles
  • Pyrimidines
  • Radiation-Sensitizing Agents
  • indole
  • Benzene