2. Academic Validation
  3. Novel, Broad Spectrum Anti-Cancer Agents Containing the Tricyclic 5:7:5-Fused Diimidazodiazepine Ring System

Novel, Broad Spectrum Anti-Cancer Agents Containing the Tricyclic 5:7:5-Fused Diimidazodiazepine Ring System

  • ACS Med Chem Lett. 2010 Dec 31;2(3):252-256. doi: 10.1021/ml100281b.
Atul Kondaskar 1,  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
Affiliations

Affiliation

  • 1 Laboratory for Drug Design & Synthesis, Department of Chemistry & Biochemistry, University of Maryland, Baltimore County, 1000 Hilltop Circle, Baltimore, Maryland, 21250, USA.
PMID: 21572541 DOI: 10.1021/ml100281b
Abstract

Synthesis of a series of novel, broad-spectrum anti-cancer 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 IC(50)'s 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.

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