Structure-activity relationship studies on thiaplidiaquinones A and B as novel inhibitors of Plasmodium falciparum and farnesyltransferase

[Display omitted] Marine meroterpenoids, thiaplidiaquinones A and B and their respective non-natural dioxothiazine regioisomers have been shown to inhibit mammalian and protozoal farnesyltransferase (FTase) with the regioisomers exhibiting activity in the nanomolar range. In order to explore the str...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2017-08, Vol.25 (16), p.4433-4443
Hauptverfasser:	Cadelis, Melissa M., Bourguet-Kondracki, Marie-Lise, Dubois, Joëlle, Kaiser, Marcel, Brunel, Jean Michel, Barker, David, Copp, Brent R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Anti-plasmodial Antimalarials - chemical synthesis Antimalarials - chemistry Antimalarials - pharmacology Biochemistry, Molecular Biology Biomimetic Cell Line Cell Survival - drug effects Dose-Response Relationship, Drug Farnesyltranstransferase - antagonists & inhibitors Farnesyltranstransferase - metabolism FTase inhibitor Life Sciences Microbial Sensitivity Tests Molecular biology Molecular Structure Natural product Plasmodium falciparum - drug effects Plasmodium falciparum - enzymology Rats Staphylococcus - classification Staphylococcus - drug effects Structure-Activity Relationship Terpenes - chemical synthesis Terpenes - chemistry Terpenes - pharmacology Thiaplidiaquinone
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