Author(s): Merckl L, Dubois J, Place E, Thoret S, Guritte F,
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Abstract Two novel 5(20)-thia analogues of docetaxel have been synthesized from 10-deacetylbaccatin III or taxine B and isotaxine B. The key step of these syntheses is the concomitant thietane ring formation and acetylation of the tertiary alcohol at C-4. Both compounds are less cytotoxic than docetaxel but have divergent activity on microtubule disassembly.
This article was published in J Org Chem
and referenced in Medicinal Chemistry