title: Novel, Broad Spectrum Anti-Cancer Agents Containing the Tricyclic 5:7:5-Fused Diimidazodiazepine Ring System.
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.
authors.affiliation: Laboratory for Drug Design & Synthesis, Department of Chemistry & Biochemistry, University of Maryland, Baltimore County, 1000 Hilltop Circle, Baltimore, Maryland, 21250, USA.
authors.forename: Atul
authors.initials: A
authors.lastname: Kondaskar
authors.forename: Shilpi
authors.initials: S
authors.lastname: Kondaskar
authors.forename: Raj
authors.initials: R
authors.lastname: Kumar
authors.forename: James C
authors.initials: JC
authors.lastname: Fishbein
authors.forename: Nidal
authors.initials: N
authors.lastname: Muvarak
authors.forename: Rena G
authors.initials: RG
authors.lastname: Lapidus
authors.forename: Mariola
authors.initials: M
authors.lastname: Sadowska
authors.forename: Martin J
authors.initials: MJ
authors.lastname: Edelman
authors.forename: Guus M
authors.initials: GM
authors.lastname: Bol
authors.forename: Farhad
authors.initials: F
authors.lastname: Vesuna
authors.forename: Venu
authors.initials: V
authors.lastname: Raman
authors.forename: Ramachandra S
authors.initials: RS
authors.lastname: Hosmane