TY - JOUR
T1 - Oxo-heterocyclic fused naphthalimides as antitumor agents
T2 - Synthesis and biological evaluation
AU - Tan, Shaoying
AU - Yin, Hong
AU - Chen, Zhuo
AU - Qian, Xuhong
AU - Xu, Yufang
PY - 2013/4
Y1 - 2013/4
N2 - Three series of novel oxo-heterocyclic fused naphthalimide derivatives (8a-8f, 13a-13d, 17a-17d) were prepared. The newly-synthesized compounds, and their thio-heterocyclic fused analogs (1a-1c, 2a-2d, 3a-3c) exhibited potent antiproliferative activity correlated well with their structure. Further research demonstrated that all the representative compounds 13a, 2a and 17a, 3a showed strong inhibition activity to topo II similarly with amonafide, and also potent topo I inhibition activity, which was seldom reported before for naphthalimide derivatives. Preliminary exploration proved their DNA sequence preference. In all, dual topo I/topo II inhibition and DNA sequence preference might contribute to enhancing tumor selectivity and overcoming drug resistance.
AB - Three series of novel oxo-heterocyclic fused naphthalimide derivatives (8a-8f, 13a-13d, 17a-17d) were prepared. The newly-synthesized compounds, and their thio-heterocyclic fused analogs (1a-1c, 2a-2d, 3a-3c) exhibited potent antiproliferative activity correlated well with their structure. Further research demonstrated that all the representative compounds 13a, 2a and 17a, 3a showed strong inhibition activity to topo II similarly with amonafide, and also potent topo I inhibition activity, which was seldom reported before for naphthalimide derivatives. Preliminary exploration proved their DNA sequence preference. In all, dual topo I/topo II inhibition and DNA sequence preference might contribute to enhancing tumor selectivity and overcoming drug resistance.
KW - Antitumor agents
KW - DNA intercalation
KW - Naphthalimides
KW - Oxo-heterocyclic
KW - Topo I
KW - Topo II
UR - https://www.scopus.com/pages/publications/84872685443
U2 - 10.1016/j.ejmech.2012.12.039
DO - 10.1016/j.ejmech.2012.12.039
M3 - 文章
C2 - 23353750
AN - SCOPUS:84872685443
SN - 0223-5234
VL - 62
SP - 130
EP - 138
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -