TY - JOUR
T1 - Novel efficient anticancer agents and DNA-intercalators of 1,2,3-triazol-1,8-naphthalimides
T2 - Design, synthesis, and biological activity
AU - Li, Xiaolian
AU - Lin, Yanjie
AU - Yuan, Yukun
AU - Liu, Kai
AU - Qian, Xuhong
PY - 2011/3/25
Y1 - 2011/3/25
N2 - Two novel series of 3-1,2,3-triazol-1,8-naphthalimides 5a-e, 7a-e were synthesized easily by employing 'click reaction'. Their bioactivities were evaluated. Compounds 5a-e were found to be more toxic against MCF-7 cells while 7a-e were more potent against 7721 cells, in particular 7a, the IC50 value of which against cell lines of MCF-7 and 7721 was 0.348 μM and 0.258 μM, respectively. Due to the phenyl group linked to 1,2,3-triazole, compound 5a not only showed higher DNA affinity but also more efficient DNA damaging ability than compound 7a.
AB - Two novel series of 3-1,2,3-triazol-1,8-naphthalimides 5a-e, 7a-e were synthesized easily by employing 'click reaction'. Their bioactivities were evaluated. Compounds 5a-e were found to be more toxic against MCF-7 cells while 7a-e were more potent against 7721 cells, in particular 7a, the IC50 value of which against cell lines of MCF-7 and 7721 was 0.348 μM and 0.258 μM, respectively. Due to the phenyl group linked to 1,2,3-triazole, compound 5a not only showed higher DNA affinity but also more efficient DNA damaging ability than compound 7a.
KW - Anticancer
KW - Intercalation
KW - Naphthalimides
KW - Triazole
UR - https://www.scopus.com/pages/publications/79952189228
U2 - 10.1016/j.tet.2011.01.063
DO - 10.1016/j.tet.2011.01.063
M3 - 文章
AN - SCOPUS:79952189228
SN - 0040-4020
VL - 67
SP - 2299
EP - 2304
JO - Tetrahedron
JF - Tetrahedron
IS - 12
ER -