Molecular design, chemical synthesis, and biological evaluation of '4-1' pentacyclic aryl/heteroaryl-imidazonaphthalimides.
A novel series of '4-1' pentacyclic naphthalimides, where the chromophore consists of a naphthalimide moiety, fused to an imidazole ring containing an unfused aryl or heteroaryl ring, were synthesized and evaluated for in vitro antitumor activity. In general, the new derivatives showed an improved cytotoxic activity over amonafide. DNA binding experiments supported that this class of compounds behaves as effective DNA-intercalating agents.
Li
Feng
F
State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian, China.
Cui
Jingnan
J
Guo
Lianying
L
Qian
Xuhong
X
Ren
Weimin
W
Wang
Kewei
K
Liu
Fengyu
F
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004247:DNA / Q000737:chemistry; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D053644:Naphthalimides / Q000737:chemistry* / Q000494:pharmacology*; D013056:Spectrophotometry, Ultraviolet; D013329:Structure-Activity Relationship; D044366:Transition Temperature
D000970:Antineoplastic Agents; D053644:Naphthalimides; D004247:DNA