Total Synthesis-Enabled Systematic Structure-Activity Relationship Study for Development of a Bioactive Alkyne-Tagged Derivative of Neolaxiflorin L

Mengxun Zhang, Magnolia Muk Lan Lee, Weijian Ye, Wing Yan Wong, Brandon Dow Chan, Sibao Chen*, Lizhi Zhu, William C S TAI, Chi Sing LEE

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)

Abstract

Neolaxiflorin L (NL) is a low-abundant Isodon 7,20-epoxy-ent-kuarenoid and was found to be a promising anticancer drug candidate in our previous study. In order to study its structure-activity relationship (SAR), a diversity-oriented synthetic route toward two libraries of (±)-NL analogs, including analogs containing different functionalities in the same 7,20-epoxy-ent-kuarene skeleton and analogs with skeletal changes, has been developed. The results of this total synthesis-enabled SAR successfully led to a bioactive alkyne-tagged NL derivative, which could be a useful probe for proteomics studies.

Original languageEnglish
Pages (from-to)7007-7016
Number of pages10
JournalJournal of Organic Chemistry
Volume84
Issue number11
DOIs
Publication statusPublished - 7 Jun 2019

Scopus Subject Areas

  • Organic Chemistry

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