Bis-naphthalimides: a new class of antitumor agents.
A series of bis-intercalators bearing the 1,8-naphthalimide chromophore has been synthesized and in vitro activities determined. Most compounds have higher activities in HT-29 than the leader compounds Mitonafide and Amonafide. One of them (22) was selected for in vivo studies and presents an interesting activity in MX-1 and OVCAR models. (22) also acts as antitopoisomerase II.
Braña
M F
MF
Laboratorios Knoll S. A, Madrid, Spain.
Castellano
J M
JM
Morán
M
M
Pérez de Vega
M J
MJ
Romerdahl
C R
CR
Qian
X D
XD
Bousquet
P
P
Emling
F
F
Schlick
E
E
Keilhauer
G
G
D000225:Adenine; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007094:Imides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007364:Intercalating Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D053644:Naphthalimides; D009374:Neoplasms, Experimental / Q000188:drug therapy; D063065:Organophosphonates; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000970:Antineoplastic Agents; D007094:Imides; D007364:Intercalating Agents; D007546:Isoquinolines; D009281:Naphthalenes; D053644:Naphthalimides; D063065:Organophosphonates; C019215:mitonafide; C037020:amonafide; D000225:Adenine