Synthesis and cytotoxicity of gossypol related compounds.
Gossypol, gossypolone, reduced gossypol and new Schiff's bases of racemic gossypol and gossypolone were extracted or synthesized. Their cytotoxic activities on KB human cancer cells were determined. Gossypolone and the ethylamine derivative of gossypolone were the most active compounds (IC(50) in the micromolar range in both cases). The cytotoxicity of gossypol and gossypolone was increased when the tests were performed in the absence of serum and decreased when catalase as well as mannitol were added to the culture medium.
Dao
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Institut de chimie des substances naturelles, CNRS, 91198, Gif sur Yvette, France.
Gaspard
C
C
Mayer
M
M
Werner
G H
GH
Nguyen
S N
SN
Michelot
R J
RJ
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002374:Catalase / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D016895:Culture Media, Serum-Free; D004354:Drug Screening Assays, Antitumor; D016166:Free Radical Scavengers / Q000494:pharmacology; D006072:Gossypol / Q000031:analogs & derivatives / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008353:Mannitol / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D016895:Culture Media, Serum-Free; D016166:Free Radical Scavengers; D008353:Mannitol; C043259:gossypolone; D002374:Catalase; D006072:Gossypol