Synthesis and biological evaluation of simplified mycothiazole analogues.
Thiazoline and oxazoline analogues of the natural product mycothiazole were synthesized from a common intermediate and evaluated in vitro against HCT-15 colon cancer cells and L(4) larvae of nematode Nippostrongylus brasiliensis. The nature of the heterocyclic moiety seems to modulate the cytotoxic or anthelmintic activity.
Mahler
Graciela
G
Departamento de Química Orgánica, Cátedra de Química Farmacéutica Facultad de Química, Universidad de la República, Montevideo, Uruguay.
Serra
Gloria
G
Dematteis
Sylvia
S
Saldaña
Jenny
J
Domínguez
Laura
L
Manta
Eduardo
E
D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D045744:Cell Line, Tumor; D007814:Larva / Q000187:drug effects; D015394:Molecular Structure; D009559:Nippostrongylus / Q000187:drug effects; D010081:Oxazolone / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity
D000871:Anthelmintics; D013844:Thiazoles; C508681:mycothiazole; C461065:trifluoromethyloxazolinone; D010081:Oxazolone