The total synthesis of an aurone isolated from Uvaria hamiltonii: aurones and flavones as anticancer agents.

Lawrence, Nicholas J; Rennison, David; McGown, Alan T; Hadfield, John A

Lawrence, Nicholas J; Rennison, David; McGown, Alan T; Hadfield, John A.

Affiliation

Lawrence NJ; Department of Chemistry, Cardiff University, PO Box 912, Cardiff CF10 3TB, UK. lawrencenj1@cardiff.ac.uk

Bioorg Med Chem Lett ; 13(21): 3759-63, 2003 Nov 03.

Article in En | MEDLINE | ID: mdl-14552774

ABSTRACT

ABSTRACT

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.

Subject(s)

Antineoplastic Agents, Phytogenic/chemical synthesis; Antineoplastic Agents, Phytogenic/pharmacology; Benzofurans/chemical synthesis; Benzofurans/pharmacology; Flavonoids/chemical synthesis; Flavonoids/pharmacology; Uvaria/chemistry; Antineoplastic Agents, Phytogenic/isolation & purification; Benzofurans/isolation & purification; Cell Cycle/drug effects; DNA, Neoplasm/drug effects; G2 Phase/drug effects; Humans; Indicators and Reagents; K562 Cells; Mitosis/drug effects; Models, Molecular; Molecular Conformation; Protein Binding; Structure-Activity Relationship; Tetrazolium Salts; Thiazoles; Tubulin/drug effects; Tubulin/metabolism

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Collection: 01-internacional Database: MEDLINE Main subject: Benzofurans / Flavonoids / Uvaria / Antineoplastic Agents, Phytogenic Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2003 Type: Article Affiliation country: United kingdom

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