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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.

Reddy YT, Sekhar KR, Sasi N, Reddy PN, Freeman ML, Crooks PA
Bioorg Med Chem Lett. 2010 20 (2): 600-2

PMID: 20005706 · PMCID: PMC4159675 · DOI:10.1016/j.bmcl.2009.11.082

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.

Copyright 2009 Elsevier Ltd. All rights reserved.

MeSH Terms (8)

Antineoplastic Agents Barbiturates Benzene HT29 Cells Humans Indoles Pyrimidines Radiation-Sensitizing Agents

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