Epothilones have captured the attention of chemists, biologists, and drug researchers ever since they were found to inhibit human cancer cell growth through a “taxol‐like” mechanism over ten years ago. Today, at least seven epothilone‐derived agents have entered clinical trials. However, additional new and exciting analogues have emerged in recent years, suggesting that the potential of these natural products to serve as leads for new anticancer drugs is far from exhausted.

De novo designed and synthesized methylthiopyrazole epothilone B boasts a stunning biological profile against tumor cells, with activity at sub‐nanomolar (IC50=0.06 nm) concentrations.

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PFEIFFER, B.; ARSENIYADIS, S.; PRATT, B. A.; NICOLAOU, K. C.; ChemMedChem 2 (2007) 4, 397-423; Dep. Chem. Appl. Biosci., ETH-Hoenggerberg, CH-8093 Zuerich, Switz.; Eng.) -Lindner 28-239