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Title: Synthesis and evaluation of novel anticancer compounds derived from the natural product brevilin A
Authors: Lee, MML 
Chan, BD 
Wong, WY 
Leung, TW 
Qu, Z 
Huang, JR
Zhu, LZ
Lee, CS
Chen, SB 
Tai, WCS 
Issue Date: 2020
Source: ACS omega, 2020, v. 5, no. 24, p. 14586-14596
Abstract: Cancer is the second leading cause of death globally, responsible for an estimated 9.6 million deaths in 2018, and this burden continues to increase. Therefore, there is a clear and urgent need for novel drugs with increased efficacy for the treatment of different cancers. Previous research has demonstrated that brevilin A (BA) exerts anticancer activity in various cancers, including human multiple myeloma, breast cancer, lung cancer, and colon carcinoma, suggesting the anticancer potential present in the chemical scaffold of BA. Here, we designed and synthesized a small library of 12 novel BA derivatives and evaluated the biological anticancer effects of the compounds in various cancer cell lines. The results of this structure-activity relationship study demonstrated that BA derivatives BA-9 and BA-10 possessed significantly improved anticancer activity toward lung, colon, and breast cancer cell lines. BA-9 and BA-10 could more effectively reduce cancer cell viability and induce DNA damage, cell-cycle arrest, and apoptosis when compared with BA. Our findings represent a significant step forward in the development of novel anticancer entities.
Publisher: American Chemical Society
Journal: ACS omega 
ISSN: 2470-1343
DOI: 10.1021/acsomega.0c01276
Rights: © 2020 American Chemical Society
This is an open access article published under an ACS AuthorChoice License (, which permits copying and redistribution of the article or any adaptations for non-commercial purposes.
The following publication Lee, M. M. L., Chan, B. D., Wong, W. Y., Leung, T. W., Qu, Z., Huang, J. R., . . . Tai, W. C. S. (2020). Synthesis and evaluation of novel anticancer compounds derived from the natural product brevilin A. Acs Omega, 5(24), 14586-14596 is available at
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