Synthesis and Evaluation of Novel Anticancer Compounds Derived from the Natural Product Brevilin A

Magnolia Muk Lan Lee, Brandon Dow Chan, Wing Yan Wong, Tsz Wing Leung, Zhao Qu, Junrong Huang, Lizhi Zhu, Chi Sing LEE, Sibao Chen*, William C S TAI

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

2 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)14586-14596
Number of pages11
JournalACS Omega
Volume5
Issue number24
DOIs
Publication statusPublished - 23 Jun 2020

Scopus Subject Areas

  • Chemistry(all)
  • Chemical Engineering(all)

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