2. Academic Validation
  3. Synthesis and cytotoxic activity of novel 10-alkylated docetaxel analogs

Synthesis and cytotoxic activity of novel 10-alkylated docetaxel analogs

  • Bioorg Med Chem Lett. 1998 Mar 3;8(5):427-32. doi: 10.1016/s0960-894x(98)00040-7.
K Nakayama 1,  H Terasawa,  I Mitsui,  S Ohsuki,  K Uoto,  S Iimura,  T Soga
Affiliations

Affiliation

  • 1 New Product Research Laboratories IV, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
PMID: 9871592 DOI: 10.1016/s0960-894x(98)00040-7
Abstract

An alkylation method of docetaxel at the C-10 position has been established by a radical coupling reaction using a 10-xanthate derivative of 7-O-TES-10-deacetylbaccatin III and appropriate alkenes. In addition the cytotoxic activity of 10-alkylated docetaxel analogs was evaluated. Among these analogs, a derivative having a methoxycarbonyl group at the end of the alkyl moiety exhibited more potent cytotoxic activity than docetaxel.

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