2. Academic Validation
  3. Synthesis and biological evaluation of novel triptolide analogues for anticancer activity

Synthesis and biological evaluation of novel triptolide analogues for anticancer activity

  • Bioorg Med Chem Lett. 2010 Nov 1;20(21):6217-21. doi: 10.1016/j.bmcl.2010.08.106.
Bing Zhou 1,  Zehong Miao,  Gang Deng,  Jian Ding,  Yaxi Yang,  Huijin Feng,  Yuanchao Li
Affiliations

Affiliation

  • 1 Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Road Zu Chong Zhi, Zhangjiang Hi-Tech Park, Shanghai 201203, PR China.
PMID: 20833543 DOI: 10.1016/j.bmcl.2010.08.106
Abstract

Three types of novel triptolide analogues with 9,11-olefin (3-5), five-membered unsaturated lactam ring (6-7) or A/B cis ring junction (8-14) were synthesized. Although with 9,11-olefin instead of 9,11-β-epoxide, compound 4a was much more active than the parent natural triptolide (1) with the lowest IC(50) value of 0.05nM for SKOV-3 cells, clearly challenging the traditional viewpoint on the necessity of 9,11-β-epoxide group of triptolide. In addition, structure-activity relationships for three classes of compounds were studied.

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