Synthesis of Analogues of Paclitaxel with 14β-Side Chain from Sinenxan A

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Synthesis of Analogues of Paclitaxel with 14β-Side Chain from Sinenxan A

Yin Dali, Liu Ruiwu, Wang Donghui, Guo Jiyu, Liang Xiaotian^*, Yoshinori Sekiguchi, Kazuya Kameo

1.Institute of Materia Medica, China Academy of Medical Sciences acd Peking Union Medical College, Beijing 100050;
2.Taisho Pharmaceutical Co.Lid 403 Youshion-Cho 1-Chome Ohmiya-shi, Saitama, 330, Japan

Received:1998-12-14 Revised:1999-06-03 Online:1999-12-15 Published:1999-12-15
Contact: Liang Xiaotian*

Abstract

Abstract: Sinenxan A (2), isolated from tissue culture, possesses an A/B/C ring skeletonwithout 1,7,9,13-oxygen functionality of paclitaxel (1). Two 1,7,9,13-deoxy, C-14β side chain analogues 4 and 5 of 1 were synthesized from 2 by incorporating the 4,20-double bond into the D-ring and introducing the side chain at 14β position. Compounds 4 and 5 showed significantly decreasedactivity in the cytotoxicity assay in vitro against KB, A2780, and HCT-8. In tubulin assembly assaythey did not show any activity at 10 μmol.L^-1.

Key words: Sinenxan A, Sinenxan A, C-14β side chain paclitaxel analogues, C-14β side chain paclitaxel analogues, Semisynthesis, Semisynthesis

Supporting:

Yin Dali, Liu Ruiwu, Wang Donghui, Guo Jiyu, Liang Xiaotian^*, Yoshinori Sekiguchi, Kazuya Kameo. Synthesis of Analogues of Paclitaxel with 14β-Side Chain from Sinenxan A[J]. .

Synthesis of Analogues of Paclitaxel with 14β-Side Chain from Sinenxan A

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