Synthesis and biological evaluation of cytotoxic properties of stilbene-based resveratrol analogs.
This work deals with the preparation of stilbene-based resveratrol analogs by employing the Perkin reaction, aiming at synthesizing potential antitumor lead compounds and evaluating their pharmacological activities. The proliferation inhibitor test against tumor cell lines identified analogs 9 and 11 as the most active among all synthesized derivatives, presenting IC(50) in micromolar range for certain cell lines. For study on the embryonic development, compounds 8 and 9 at the lowest tested concentration (41.7 microM) that inhibited sea urchin egg development, but only after third cleavage were used. Both the compounds inhibited 100% of normal development since first cleavage. These data partially corroborated the results obtained with MTT assay using tumor cell lines. None of the tested compounds revealed hemolytic action in assay with mouse erythrocytes.
de Lima
Dênis Pires
DP
Departamento de Química, Universidade Federal de Mato Grosso do Sul, CP 549, 79070-900 Campo Grande, MS, Brazil. dlima@nin.ufms.br
Rotta
Rodrigo
R
Beatriz
Adilson
A
Marques
Maria Rita
MR
Montenegro
Raquel C
RC
Vasconcellos
Marne C
MC
Pessoa
Cláudia
C
de Moraes
Manoel O
MO
Costa-Lotufo
Letícia V
LV
Frankland Sawaya
Alexandra Christine Helena
AC
Eberlin
Marcos Nogueira
MN
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D047108:Embryonic Development / Q000187:drug effects; D004912:Erythrocytes / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D010063:Ovum; D000077185:Resveratrol; D012617:Sea Urchins; D013267:Stilbenes / Q000138:chemical synthesis* / Q000494:pharmacology
D000970:Antineoplastic Agents; D013267:Stilbenes; D000077185:Resveratrol