title: Synthesis and SERCA activities of structurally simplified cyclopiazonic acid analogues.
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.
authors: Bergische Universität Wuppertal, Fachgruppe Chemie, Gaußstraße 20, D-42119 Wuppertal, Germany.
authors: Sheng
authors: S
authors: Yao
authors: Daniel
authors: D
authors: Gallenkamp
authors: Katharina
authors: K
authors: Wölfel
authors: Bettina
authors: B
authors: Lüke
authors: Michael
authors: M
authors: Schindler
authors: Jürgen
authors: J
authors: Scherkenbeck
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008958:Models, Molecular; D009036:Moths / Q000201:enzymology*; D053498:Sarcoplasmic Reticulum Calcium-Transporting ATPases / Q000037:antagonists & inhibitors* / Q000378:metabolism*
chemical_list: D004791:Enzyme Inhibitors; D007211:Indoles; D053498:Sarcoplasmic Reticulum Calcium-Transporting ATPases; C000543:cyclopiazonic acid