[Studies on anti-tumor agents. I: Synthesis and anti-cancer activity of amino acid derivatives of norcantharidin].
In order to search for new compounds with higher anti-cancer activities and lower toxicities, 19 amino acid derivatives of norcantharidin, of which 16 are unknown compounds, were designed and synthesized. Preliminary screening results revealed that 2-(syn-exo-7-oxabicyclo [2.2.1] heptane-2,3-dicarboxylic imido)-N-phenyl glutaramic acid exhibited a fairly apparent inhibitory activity against human-hepatoma cells in vitro (inhibitory rate 39.4% at 0.025 mumol/ml).
Tian
S L
SL
National Institutes of Pharmaceutical Research & Development, Beijing.
Zhao
S W
SW
Zhu
A T
AT
Fang
Y
Y
Li
K Q
KQ
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D019086:Bridged Bicyclo Compounds, Heterocyclic; D006528:Carcinoma, Hepatocellular / Q000473:pathology; D006801:Humans; D008113:Liver Neoplasms / Q000473:pathology; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000970:Antineoplastic Agents; D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; C069741:norcantharidin