TY - JOUR
T1 - Synthesis of 7-triazole-substituted camptothecin via click chemistry and evaluation of in vitro antitumor activity
AU - Wang, Lei
AU - Yuan, Wei
AU - Zhang, Jie
AU - Tong, Linjiang
AU - Luo, Yu
AU - Chen, Yi
AU - Lu, Wei
AU - Huang, Qingqing
PY - 2014/2
Y1 - 2014/2
N2 - Camptothecin (CPT) is a natural topoisomerase I inhibitor with powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers. To discover more potent antitumor agents, a series of new CPT derivatives were synthesized utilizing click chemistry. All compounds were assessed for cytotoxicity against A549, HCT-116, HT-29, LoVo, MDA-MB-231 cell lines, and some compounds exhibited good in vitro potency. Furthermore, all compounds kept or enhanced Topo I inhibition. A series of novel 7-triazole substituted camptothecin via click chemistry was designed, synthesized, and evaluated for their in vitro antitumor activity.
AB - Camptothecin (CPT) is a natural topoisomerase I inhibitor with powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers. To discover more potent antitumor agents, a series of new CPT derivatives were synthesized utilizing click chemistry. All compounds were assessed for cytotoxicity against A549, HCT-116, HT-29, LoVo, MDA-MB-231 cell lines, and some compounds exhibited good in vitro potency. Furthermore, all compounds kept or enhanced Topo I inhibition. A series of novel 7-triazole substituted camptothecin via click chemistry was designed, synthesized, and evaluated for their in vitro antitumor activity.
KW - 7-triazole-substituted camptothecin
KW - antitumor
KW - camptothecin
KW - click chemistry
UR - https://www.scopus.com/pages/publications/84894498565
U2 - 10.1002/cjoc.201300703
DO - 10.1002/cjoc.201300703
M3 - 文章
AN - SCOPUS:84894498565
SN - 1001-604X
VL - 32
SP - 157
EP - 162
JO - Chinese Journal of Chemistry
JF - Chinese Journal of Chemistry
IS - 2
ER -
