Synthesis and evaluation of pyrazolignans. A new class of cytotoxic agents.
A series of fused pyrazole derivatives of cyclolignans have been prepared through simple chemical routes and evaluated for their cytotoxic activities in culture cells of P-388 murine leukemia, A-549 lung carcinoma and HT-29 colon carcinoma. Despite the lack of the lactone moiety in their structures, they show IC50 values at microM levels.
Gordaliza
M
M
Laboratorio de Química Farmacéutica, Facultad de Farmacia, Universidad de Salamanca, Spain.
del Corral
J M
JM
Castro
M A
MA
López-Vázquez
M L
ML
San Feliciano
A
A
García-Grávalos
M D
MD
Carpy
A
A
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D019073:HT29 Cells / Q000187:drug effects; D006801:Humans; D007941:Leukemia P388 / Q000188:drug therapy; D017705:Lignans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008175:Lung Neoplasms / Q000188:drug therapy; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D051379:Mice; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000972:Antineoplastic Agents, Phytogenic; D017705:Lignans; D011720:Pyrazoles