Structure activity studies of a novel cytotoxic benzodiazepine

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Abstract

Analogues of Bz-423, a pro-apoptotic 1,4-benzodiazepine with potent activity in animal models of systemic lupus erythematosus and rheumatoid arthritis, have been designed, synthesized, and evaluated in cell-culture assays. The results of these experiments have defined the structural elements of this new cytotoxic agent required for activity.

Analogues of Bz-423, a pro-apoptotic 1,4-benzodiazepine active in animal models of lupus and rheumatoid arthritis, have been designed, synthesized, and evaluated in cell culture assays. These experiments have defined the structural elements of this new cytotoxic agent required for activity.

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Acknowledgements

This research was supported by NIH grants AI-47450 and GM-42168 (to G.D.G.), GM-50353 (to J.A.E.), and AI 35709 (to W.R.R). The authors thank J. Patchett for the synthesis of 18.

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