Jump to main content
Jump to site search
Access to RSC content Close the message box

Continue to access RSC content when you are not at your institution. Follow our step-by-step guide.


Issue 11, 2017
Previous Article Next Article

Design, synthesis and structure–activity relationships of (±)-isochaihulactone derivatives

Author affiliations

Abstract

Z-K8 (2), the racemic form of isochaihulactone (1), previously showed significant antitumor effects in A549 and LNCaP tumor-bearing mice. In the present study, 17 derivatives of 2 were designed, synthesized and evaluated for their anti-proliferative activity against four human tumor cell lines. All new derivatives exhibited high potency against A549 and P-glycoprotein (P-gp)-overexpressing KB-VIN. One of our new derivatives exhibited greater activity against three tested tumor cells (A549, KB, and KB-VIN) than 2, and induced cell cycle arrest in the G2/M phase. Moreover, SAR conclusions were first established for this series of compounds. Our study clearly identified a structural feature that should be retained for good activity and also a moiety that can tolerate various modifications and, thus, is ideal for further changes.

Graphical abstract: Design, synthesis and structure–activity relationships of (±)-isochaihulactone derivatives

Back to tab navigation

Article information


Submitted
21 Jun 2017
Accepted
15 Sep 2017
First published
12 Oct 2017

Med. Chem. Commun., 2017,8, 2040-2049
Article type
Research Article

Design, synthesis and structure–activity relationships of (±)-isochaihulactone derivatives

Y. Zhao, P. Liu, K. Hsieh, P. Hsu, M. Goto, S. L. Morris-Natschke, H. Harn and K. Lee, Med. Chem. Commun., 2017, 8, 2040
DOI: 10.1039/C7MD00310B

Search articles by author

Spotlight

Advertisements