Abstract
Natural products of the naphthoquinone spiroketal structural type served as lead structures for the development of novel inhibitors of the thioredoxin-thioredoxin reductase redox system. The most potent compound in this series inhibited thioredoxin with an IC(50) of 350 nM, and many derivatives showed low micromolar activities for growth inhibition against two breast cancer cell lines.
Publication types
-
Research Support, Non-U.S. Gov't
-
Research Support, U.S. Gov't, Non-P.H.S.
-
Research Support, U.S. Gov't, P.H.S.
MeSH terms
-
Antineoplastic Agents / chemical synthesis
-
Antineoplastic Agents / chemistry
-
Antineoplastic Agents / pharmacology
-
Cell Division / drug effects
-
Dioxanes / chemical synthesis
-
Dioxanes / chemistry
-
Dioxanes / pharmacology
-
Drug Screening Assays, Antitumor
-
Epoxy Compounds / chemical synthesis
-
Epoxy Compounds / chemistry
-
Epoxy Compounds / pharmacology
-
Humans
-
Naphthalenes
-
Naphthoquinones / chemical synthesis
-
Naphthoquinones / chemistry
-
Naphthoquinones / pharmacology*
-
Spiro Compounds / chemical synthesis
-
Spiro Compounds / chemistry
-
Spiro Compounds / pharmacology
-
Thioredoxin-Disulfide Reductase / antagonists & inhibitors*
-
Thioredoxins / antagonists & inhibitors*
-
Tumor Cells, Cultured
Substances
-
Antineoplastic Agents
-
Dioxanes
-
Epoxy Compounds
-
Naphthalenes
-
Naphthoquinones
-
Spiro Compounds
-
diepoxin sigma
-
palmarumycin CP(1)
-
Thioredoxins
-
Thioredoxin-Disulfide Reductase