2. Academic Validation
  3. Synthesis and SERCA activities of structurally simplified cyclopiazonic acid analogues

Synthesis and SERCA activities of structurally simplified cyclopiazonic acid analogues

  • Bioorg Med Chem. 2011 Aug 1;19(15):4669-78. doi: 10.1016/j.bmc.2011.06.001.
Sheng Yao 1,  Daniel Gallenkamp,  Katharina Wölfel,  Bettina Lüke,  Michael Schindler,  Jürgen Scherkenbeck
Affiliations

Affiliation

  • 1 Bergische Universität Wuppertal, Fachgruppe Chemie, Gaußstraße 20, D-42119 Wuppertal, Germany.
PMID: 21719297 DOI: 10.1016/j.bmc.2011.06.001
Abstract

The indole alkaloid cyclopiazonic acid (CPA) is one of the few known nanomolar inhibitors of sarco(endo)plasmic reticulum Ca²⁺-ATPase (SERCA) besides the Anticancer drug thapsigargin and the antiplasmoidal terpenoid artemisinin. Due to its less complex structure CPA represents an attractive lead structure for the development of novel antimalarial drugs or for applications in the field of plant protection. We report here the first syntheses of structurally simplified CPA fragments and discuss their SERCA activities on the basis of published crystal structures of CPA-SERCA complexes.

Figures