Issue 29, 2013

Design and biological characterization of hybrid compounds of curcumin and thalidomide for multiple myeloma

Abstract

In our efforts to develop effective treatment agents for human multiple myeloma (MM), a series of hybrid molecules based on the structures of thalidomide (1) and curcumin (2) were designed, synthesized, and biologically characterized in human multiple myeloma MM1S, RPMI8226, U266 cells, and human lung cancer A549 cells. The biological results showed that two hybrid compounds, 5 and 7, exhibited significantly improved lethal effects towards all three human MM cell models compared to 1 or 2 alone, as well as the combination of 1 and 2. Furthermore, mechanistic studies in U266 cells demonstrated that 5 and 7 can induce the production of reactive oxygen species (ROS) and cause G1/S arrest, thus leading to apoptosis and cell death. Additionally, they exhibited inhibitory effects on NFκB activation in A549 cells. Collectively, the results obtained from these hybrid compounds strongly encourage their further optimization as new leads to develop effective treatment agents for human MM.

Graphical abstract: Design and biological characterization of hybrid compounds of curcumin and thalidomide for multiple myeloma

Supplementary files

Additions and corrections

Article information

Article type
Communication
Submitted
25 Mar 2013
Accepted
07 Jun 2013
First published
11 Jun 2013

Org. Biomol. Chem., 2013,11, 4757-4763

Design and biological characterization of hybrid compounds of curcumin and thalidomide for multiple myeloma

K. Liu, D. Zhang, J. Chojnacki, Y. Du, H. Fu, S. Grant and S. Zhang, Org. Biomol. Chem., 2013, 11, 4757 DOI: 10.1039/C3OB40595H

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements