2. Academic Validation
  3. New highly active taxoids from 9beta-dihydrobaccatin-9,10-acetals. Part 2

New highly active taxoids from 9beta-dihydrobaccatin-9,10-acetals. Part 2

  • Bioorg Med Chem Lett. 2002 Oct 21;12(20):2815-9. doi: 10.1016/s0960-894x(02)00628-5.
Takashi Ishiyama 1,  Shin Iimura,  Toshiharu Yoshino,  Jun Chiba,  Kouichi Uoto,  Hirofumi Terasawa,  Tsunehiko Soga
Affiliations

Affiliation

  • 1 Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co., Ltd., Tokyo R&D Center, 16-13 Kita-kasai 1-Chome Edogawa-ku, Tokyo, Japan.
PMID: 12270153 DOI: 10.1016/s0960-894x(02)00628-5
Abstract

To investigate structure-activity relationships of the 9,10-acetal-9beta-dihydro taxoids, we modified the 7-hydroxyl groups of the 9,10-acetonide-3'-(4-pyridyl) analogue to deoxy, methoxy, alpha-F, and 7beta,8beta-methano group. As a result of this study, we found that the 7-deoxy analogue was the strongest among these analogues. In addition, we found that the 7-deoxy-3'-(4-pyridyl) and 7-deoxy-3'-(2-pyridyl) analogues showed stronger activity against cell lines expressing P-glycoprotein than the corresponding 3'-phenyl analogue.

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