Novel, broad spectrum anticancer agents containing the tricyclic 5:7:5-fused diimidazodiazepine ring system

Atul Kondaskar, Shilpi Kondaskar, Raj Kumar, James C. Fishbein, Nidal Muvarak, Rena G. Lapidus, Mariola Sadowska, Martin J. Edelman, Guus M. Bol, Farhad Vesuna, Venu Raman, Ramachandra S. Hosmane

Research output: Contribution to journalArticle

Abstract

Synthesis of a series of novel, broad spectrum anticancer agents containing the tricyclic 5:7:5-fused diimidazo[4,5-d:4′,5′-f][1,3]diazepine ring system is reported. Compounds 1, 2, 8, 11, and 12 in the series show promising in vitro antitumor activity with low micromolar IC50 values against prostate, lung, breast, and ovarian cancer cell lines. Some notions about structure-activity relationships and a possible mechanism of biological activity are presented. Also presented are preliminary in vivo toxicity studies of 1 using SCID mice.

Original languageEnglish (US)
Pages (from-to)252-256
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume2
Issue number3
DOIs
StatePublished - Mar 10 2011

Keywords

  • 5:7:5-fused tricycles
  • Synthesis
  • and ovarian cancers
  • breast
  • broad spectrum anticancer activity
  • diimidazo[4,5-d:4′,5′-f][1,3] diazepine ring system
  • effects on G1 and S phases of the cell cycle
  • in vitro screening
  • lung
  • preliminary mechanistic studies
  • prostate

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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  • Cite this

    Kondaskar, A., Kondaskar, S., Kumar, R., Fishbein, J. C., Muvarak, N., Lapidus, R. G., Sadowska, M., Edelman, M. J., Bol, G. M., Vesuna, F., Raman, V., & Hosmane, R. S. (2011). Novel, broad spectrum anticancer agents containing the tricyclic 5:7:5-fused diimidazodiazepine ring system. ACS Medicinal Chemistry Letters, 2(3), 252-256. https://doi.org/10.1021/ml100281b