Antiproliferation and apoptosis induced by C-glycosides in human leukemia cancer cells.
A large series of alkyl C-glycosides was synthesized from D-glucal or D-galactal. These compounds were screened against the human promyelocytic leukemia cell line (HL60), showing significant activity and apoptosis. Up to 13 C-glucopyranosides, but no C-galacto- or C-mannopyranosides, exhibited inhibitory concentrations (IC(50) values) below 20 microM, five of them in the range 4-8 microM. Preliminary structure-activity relationships were established.
Sanhueza
Carlos A
CA
Instituto Universitario de Bio-Orgánica Antonio González, Universidad de La Laguna, Tenerife, Spain.
Mayato
Carlos
C
García-Chicano
María
M
Díaz-Peñate
Raquel
R
Dorta
Rosa L
RL
Vázquez
Jesús T
JT
D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis; D045744:Cell Line, Tumor; D049109:Cell Proliferation; D004354:Drug Screening Assays, Antitumor; D006027:Glycosides / Q000737:chemistry*; D018922:HL-60 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D007659:Ketones; D007938:Leukemia / Q000188:drug therapy* / Q000378:metabolism* / Q000473:pathology*; D008956:Models, Chemical; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D006027:Glycosides; D007659:Ketones