4.5 Article

Calmodulin inhibitory activity of the malbrancheamides and various analogs

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 24, Pages 6479-6481

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.10.057

Keywords

Calmodulin inhibition; Malbrancheamide; Prenylated indole alkaloid

Funding

  1. National Institutes of Health [CA70375]
  2. Consejo Nacional de Ciencia y Tecnologia (CONACyT) [45814-Q]
  3. NIH Shared Instrumentation Grant at Colorado State University [GM49631]

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The preparation and biological activity of various structural analogs of the malbrancheamides are disclosed. The impact of indole chlorination, C-12a relative stereochemistry, and bicyclo[2.2.2]diazaoctane core oxidation state on the ability of these analogs to inhibit calmodulin dependent phosphodiesterase (PDE1) was studied, and a number of potent compounds were identified. [GRAPHICS] (C) 2008 Elsevier Ltd. All rights reserved.

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