The total synthesis of an aurone isolated from Uvaria hamiltonii: aurones and flavones as anticancer agents.
The naturally occurring aurone 1, isolated from Uvaria hamiltonii, and a series of aurones analogues based structurally on known tubulin binding agents were prepared and evaluated for anticancer activity. Aurone 20 was the most active (IC(50) K562 50 nM) and caused significant G2/M cell-cycle arrest.
Lawrence
Nicholas J
NJ
Department of Chemistry, Cardiff University, PO Box 912, Cardiff CF10 3TB, UK. lawrencenj1@cardiff.ac.uk
Rennison
David
D
McGown
Alan T
AT
Hadfield
John A
JA
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology*; D001572:Benzofurans / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D004273:DNA, Neoplasm / Q000187:drug effects; D005419:Flavonoids / Q000138:chemical synthesis* / Q000494:pharmacology*; D016195:G2 Phase / Q000187:drug effects; D006801:Humans; D007202:Indicators and Reagents; D020014:K562 Cells; D008938:Mitosis / Q000187:drug effects; D008958:Models, Molecular; D008968:Molecular Conformation; D011485:Protein Binding; D013329:Structure-Activity Relationship; D013778:Tetrazolium Salts; D013844:Thiazoles; D014404:Tubulin / Q000187:drug effects / Q000378:metabolism; D031046:Uvaria / Q000737:chemistry*
D000972:Antineoplastic Agents, Phytogenic; D001572:Benzofurans; D004273:DNA, Neoplasm; D005419:Flavonoids; D007202:Indicators and Reagents; D013778:Tetrazolium Salts; D013844:Thiazoles; D014404:Tubulin; C486837:aurone; C022616:thiazolyl blue