Home
Resources
Publications
Lathyrol Diterpenes as Modulators of P-glycoprotein Dependent Multidrug Resistance: Structure-Activity Relationship Studies on Euphorbia Factor L3 Derivatives

Lathyrol Diterpenes as Modulators of P-glycoprotein Dependent Multidrug Resistance: Structure-Activity Relationship Studies on Euphorbia Factor L3 Derivatives

Wei Jiao, Zhongmin Wan, Shuang Chen, Runhua Lu, Xiaozhen Chen, Dongmei Fang, Jiufeng Wang, Shengcai Pu, Xin Huang, Haixiang Gao, Huawu Shao

J Med Chem. 2015 May 14;58(9):3720-38.

PMID: 25856545

Abstract:

Five series of 37 new acylate and epoxide derivatives (3-39) of Euphorbia factor L3, a lathyrol diterpene isolated from Euphorbia lathyris, were designed by modifying the hydroxyl moiety of C-3, C-5, or C-15. Chemoreversal effects of the acylates on multidrug resistance (MDR) were evaluated in breast cancer multidrug-resistant MCF-7/ADR cells that overexpress P-glycoprotein (P-gp). Eight derivatives exhibited greater chemoreversal ability than verapamil (VRP) against adriamycin (ADR) resistance. Compounds 19 and 25 exhibited 4.8 and 4.0 times, respectively, more effective reversal ability than VRP against ADR resistance. To determine the key characteristics of Euphorbia factor L3 derivatives that contribute to MDR reversal, we conducted a structure-activity relationship study of these compounds. The simulation studies indicated different possible mechanisms and revealed the important influence of hydrophobic interactions and hydrogen bonds in the flexible cavity of P-gp.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP34420194	Lathyrol		34420-19-4	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: