Bioorganic and Medicinal Chemistry Letters p. 427 - 432 (1998)
Update date:2022-07-30
Topics:
Nakayama, Kiyoshi
Terasawa, Hirofumi
Mitsui, Ikuo
Ohsuki, Satoru
Uoto, Kouichi
Iimura, Shin
Soga, Tsunehiko
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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(1998)
