Synthesis and biological evaluation of simplified mycothiazole analogues.

Abstract

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.

• Authors: Graciela Mahler, Gloria Serra, Sylvia Dematteis, Jenny Saldaña, Laura Domínguez, Eduardo Manta
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 16 Issue 5 Pg. 1309-11 (Mar 01 2006) ISSN: 0960-894X [Print] England
• PMID: 16384701 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)

Chemical References

• Anthelmintics
• Thiazoles
• mycothiazole
• trifluoromethyloxazolinone
• Oxazolone

Topics

• Animals
• Anthelmintics (chemical synthesis, chemistry, pharmacology, toxicity)
• Cell Line, Tumor
• Larva (drug effects)
• Molecular Structure
• Nippostrongylus (drug effects)
• Oxazolone (analogs & derivatives, chemical synthesis, chemistry)
• Structure-Activity Relationship
• Thiazoles (chemical synthesis, chemistry, pharmacology, toxicity)