Design, Synthesis and Structure-Activity Relationships of (±)-Isochaihulactone Derivatives

Overview

Journal Medchemcomm

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2018 Feb 3

PMID 29391939

Citations 3

Authors

Yu Zhao

Po-Yen Liu

Kan-Yen Hsieh

Pei-Ling Hsu

Masuo Goto

Susan L Morris-Natschke

Horng-Jyh Harn

Kuo-Hsiung Lee

Affiliations

Soon will be listed here.

Abstract

Z-K8 (), the racemic form of isochaihulactone (), previously showed significant antitumor effects in A549 and LNCaP tumor-bearing mice. In the present study, 17 derivatives of , were designed, synthesized and evaluated for anti-proliferative activity against four human tumor cell lines. All new derivatives exhibited high potency against A549 and P-glycoprotein (P-gp)-overexpressing KBvin. One of our new derivative exhibited greater activity against three tested tumor cells (A549, KB, and KB-VIN) than , and induced cell cycle arrest in the G/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.

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