TY - JOUR
T1 - Design, synthesis and biological evaluation of C(6)-modified celastrol derivatives as potential antitumor agents
AU - Tang, Kaiyong
AU - Huang, Qingqing
AU - Zeng, Jafeng
AU - Wu, Guangming
AU - Huang, Jinwen
AU - Pan, Junfang
AU - Lu, Wei
PY - 2014/7
Y1 - 2014/7
N2 - New six C6-celastrol derivatives were designed, synthesized, and evaluated for their in vitro cytotoxic activities against nine human cancer cell lines (BGC-823, H4, Bel7402, H522, Colo 205, HepG2 and MDA-MB-468). The results showed that most of the compounds displayed potent inhibition against BGC823, H4, and Bel7402, with IC50s of 1.84-0.39 μM. The best compound NST001A was tested in an in vivo antitumor assay on nude mice bearing Colo 205 xenografts, and showed significant inhibition of tumor growth at low concentrations. Therefore, celastrol C-6 derivatives are potential drug candidates for treating cancer.
AB - New six C6-celastrol derivatives were designed, synthesized, and evaluated for their in vitro cytotoxic activities against nine human cancer cell lines (BGC-823, H4, Bel7402, H522, Colo 205, HepG2 and MDA-MB-468). The results showed that most of the compounds displayed potent inhibition against BGC823, H4, and Bel7402, with IC50s of 1.84-0.39 μM. The best compound NST001A was tested in an in vivo antitumor assay on nude mice bearing Colo 205 xenografts, and showed significant inhibition of tumor growth at low concentrations. Therefore, celastrol C-6 derivatives are potential drug candidates for treating cancer.
KW - Antitumor activity
KW - Celastrol C-6 derivatives
KW - In vitro
KW - In vivo
UR - https://www.scopus.com/pages/publications/84904808084
U2 - 10.3390/molecules190710177
DO - 10.3390/molecules190710177
M3 - 文章
C2 - 25025148
AN - SCOPUS:84904808084
SN - 1420-3049
VL - 19
SP - 10177
EP - 10188
JO - Molecules
JF - Molecules
IS - 7
ER -
