Cover Picture: Molecular Design and Chemical Synthesis of a Highly Potent Epothilone (ChemMedChem 1/2006)

Design, synthesis, and biological properties of highly potent epothilone B analogues.

Owing to their potent cytotoxicity against tumor cells, including taxol (paclitaxel)-resistant cell lines, the epothilones (for example, epothilone A (1) and epothilone B (2)) continue to be the focus of intense chemical, biological, and clinical research efforts around the world. 3] Following the findings that cyclopropane-, methylsulfanylthiazole-, and pyridine-containing epothilone B derivat...

Cover Picture: Targeted Fluoro Positioning for the Discovery of a Potent and Highly Selective Matrix Metalloproteinase Inhibitor (ChemistryOpen 2/2017)

Design, synthesis and biological evaluation of bridged epothilone D analogues.

Six epothilone D analogues with a bridge between the C4-methyl and the C12-methyl carbons were prepared in an attempt to constrain epothilone D to its proposed tubulin-binding conformation. Ring-closing metathesis (RCM) was employed as the key step to build the C4-C26 bridge. In antiproliferative assays in the human ovarian cancer (A2780) and prostate cancer (PC3) cell lines, and also in tubuli...

Highly Efficient CYP167A1 (EpoK) dependent Epothilone B Formation and Production of 7-Ketone Epothilone D as a New Epothilone Derivative

Since their discovery in the soil bacterium Sorangium cellulosum, epothilones have emerged as a valuable substance class with promising anti-tumor activity. Because of their benefits in the treatment of cancer and neurodegenerative diseases, epothilones are targets for drug design and pharmaceutical research. The final step of their biosynthesis - a cytochrome P450 mediated epoxidation of epoth...

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