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
N1 - Funding Information:
This work is financially supported by the National Natural Science Foundation of China (grant nos. 21502002, 21572006 21871017 and 81872769), the Natural Science Foundation of Guangdong Province, China (grant no. 2017A030313042), the Hong Kong Research Grants Council General Research Fund (project no. 12103515), the Health and Medical Research Fund (project no. 15161401), the Shenzhen Science and Technology Innovation Committee (grant nos. JCYJ20151030164022389 JCYJ20160229173844278, JCYJ20160428153421635 and JCYJ20160330095659560) Peking University Shenzhen Graduate School, Hong Kong Polytechnic University and Hong Kong Baptist University (RC-SGT2/18-19/SCI/005).
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 -
SDG 3 Good Health and Well-being