Semisynthesis and cytotoxicity of styryl-lactone derivatives.
The cytotoxicity and the cell-cycle action of altholactone (1), goniofufurone (2), and eight altholactone derivatives (5-12), were determined in vitro on L-1210 cells. Semisyntheses and structure-activity relationships of these compounds are described. The results of this study suggest that the cytotoxicity of altholactone (1), 11-nitro-altholactone (8), and 7-chloro-6,7-dihydroaltholactone (10) is due to the accumulation of the cells in the G2 + M phase of the cell cycle.
Bermejo
A
A
Departamento de Farmacología, Farmacognosia y Farmacodinamia, Facultad de Farmacia, Universidad de Valencia, 46100 Burjassot, Valencia, Spain.
Léonce
S
S
Cabedo
N
N
Andreu
I
I
Caignard
D H
DH
Atassi
G
G
Cortes
D
D
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D007783:Lactones / Q000138:chemical synthesis* / Q000494:pharmacology; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D008968:Molecular Conformation; D009512:New Guinea; D010946:Plants, Medicinal / Q000737:chemistry*; D014407:Tumor Cells, Cultured
D000972:Antineoplastic Agents, Phytogenic; D007783:Lactones