SAR studies of epoxycurcuphenol derivatives on leukemia CT-CD4 cells.
Bioactive natural products are a potential source of new pharmaceuticals since they offer new modes of action and more specific activities. The use of derivatization also enables the optimal structure for their biological activity to be determined. In this study several epoxycurcuphenol derivatives were synthesized. The substitution pattern on the aromatic and oxirane rings was varied along with that at the benzylic position and the length of the side chain was altered. These changes were made in order to gain a deeper understanding of the structural requirements for activity. The biological activities of these compounds were evaluated on the human leukemia cell line Jurkat using an antiproliferative assay. The activity results and structural requirements are discussed.
Grupo de Alelopatía, Departamento de Química Orgánica, Facultad de Ciencias, Universidad de Cádiz, C/República Saharaui s/n, Puerto Real (Cádiz), Spain.
José L G
JL
Galindo
Mariola
M
Macías
José M G
JM
Molinillo
Alba
A
Muñoz-Suano
Ascensión
A
Torres
Rosa M
RM
Varela
Francisco
F
García-Cozar
Francisco A
FA
Macías
D015496:CD4-Positive T-Lymphocytes / Q000276:immunology / Q000378:metabolism; D049109:Cell Proliferation / Q000187:drug effects; D005027:Ethylene Oxide / Q000737:chemistry; D006801:Humans; D019169:Jurkat Cells; D007938:Leukemia / Q000473:pathology; D012717:Sesquiterpenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D012717:Sesquiterpenes; C054389:curcuphenol; D005027:Ethylene Oxide