𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Synthesis and biological evaluation of novel triptolide analogues for anticancer activity

✍ Scribed by Bing Zhou; Zehong Miao; Gang Deng; Jian Ding; Yaxi Yang; Huijin Feng; Yuanchao Li

Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
672 KB
Volume
20
Category
Article
ISSN
0960-894X

No coin nor oath required. For personal study only.

✦ Synopsis

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-Ξ²-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-Ξ²-epoxide group of triptolide. In addition, structure-activity relationships for three classes of compounds were studied.

πŸ“œ SIMILAR VOLUMES

Synthesis and biological evaluation of n
Synthesis and biological evaluation of novel benzoxazinic analogues of ellipticine
✍ Deborah Mousset; RΓ©mi Rabot; Pascal Bouyssou; GΓ©rard Coudert; Isabelle Gillaizea πŸ“‚ Article πŸ“… 2010 πŸ› Elsevier Science 🌐 French βš– 680 KB

Original 1,4-benzoxazine analogues of ellipticine were prepared using a general synthetic route that relied on an anionic ring annulation as the key transformation. The interest of this approach lies on the possibility of an easy entrance to a wide range of derivatives from the phenol intermediate.