TY - JOUR
T1 - Total Synthesis-Enabled Systematic Structure-Activity Relationship Study for Development of a Bioactive Alkyne-Tagged Derivative of Neolaxiflorin L
AU - Zhang, Mengxun
AU - Lee, Magnolia Muk Lan
AU - Ye, Weijian
AU - Wong, Wing Yan
AU - Chan, Brandon Dow
AU - Chen, Sibao
AU - Zhu, Lizhi
AU - Tai, William Chi Shing
AU - Lee, Chi Sing
PY - 2019/6/7
Y1 - 2019/6/7
N2 - 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.
AB - 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.
UR - https://www.scopus.com/pages/publications/85066403580
U2 - 10.1021/acs.joc.9b00748
DO - 10.1021/acs.joc.9b00748
M3 - Journal article
C2 - 31083909
AN - SCOPUS:85066403580
SN - 0022-3263
VL - 84
SP - 7007
EP - 7016
JO - Journal of Organic Chemistry
JF - Journal of Organic Chemistry
IS - 11
ER -