Synthesis and antitumor activity of selected 7-alkylidene substituted cephems.
Selected 7-alkylidene substituted cephems were synthesized and subjected to antitumor assay. The effect of substituents was examined to establish structure-activity relationships. It was found that the intensive intracellular generation of nitric oxide induced by tert-butyl 7-alkylidene cephalosporanate sulfones could be also regarded as an additional cytotoxic factor taking place both in vitro and in vivo experiments.
Veinberg
G
G
Latvian Institute of Organic Synthesis, Riga, Latvia. veinberg@osi.lanet.lv
Vorona
M
M
Shestakova
I
I
Kanepe
I
I
Zharkova
O
O
Mezapuke
R
R
Turovskis
I
I
Kalvinsh
I
I
Lukevics
E
E
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D002511:Cephalosporins