Synthesis of novel antitumoural analogues of dysidiolide from ent-halimic acid.
Several sesterterpenolides analogues of dysidiolide have been synthesized and their in vitro antitumoural activity against human HeLa, A549, HT-29 and HL-60 carcinoma cells is presented. The proliferation inhibition data showed a significant antitumour activity of the compounds 1b, 2a, 2b, 3a, 3b, 4a, 4b, 5, inhibiting proliferation of distinct cancer cell types with an IC(50) in the low micromolar range.
Marcos
I S
IS
Departamento de Química Orgánica, Facultad de Ciencias Químicas, Universidad de Salamanca, Plaza de los Caídos 1-5, Salamanca, Spain. ismarcos@usal.es
Escola
M A
MA
Moro
R F
RF
Basabe
P
P
Diez
D
D
Sanz
F
F
Mollinedo
F
F
de la Iglesia-Vicente
J
J
Sierra
B G
BG
Urones
J G
JG
D015107:4-Butyrolactone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000447:Aldehydes / Q000737:chemistry; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D006900:Hydroxylation; D007659:Ketones / Q000737:chemistry; D008958:Models, Molecular; D015394:Molecular Structure; D054830:Sesterterpenes; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013729:Terpenes / Q000737:chemistry*
D000447:Aldehydes; D000970:Antineoplastic Agents; D007659:Ketones; D054830:Sesterterpenes; D013729:Terpenes; C004511:butenolide; C121906:dysidiolide; D015107:4-Butyrolactone