Synthesis, biological evaluation and DNA binding properties of novel mono and bisnaphthalimides.
A novel series of mono and bisnaphthalimides was synthesized and their antiproliferative activities were evaluated against three tumor cell lines. Bisnaphthalimides 3 and 4, bearing a pyrazine ring fused to the naphthalimide system, showed activities in the order of 10(-8) microM, similar to elinafide. DNA binding properties and the ability to induce DNA damage were studied for some of the most active compounds.
Braña
Miguel F
MF
Departamento de CC. Químicas, Facultad de CC. Experimentales y de la Salud, Universidad San Pablo CEU, Urb. Montepríncipe, Boadilla del Monte, 28668 Madrid, Spain.
Cacho
Mónica
M
Ramos
Ana
A
Domínguez
M Teresa
MT
Pozuelo
Jose M
JM
Abradelo
Cristina
C
Rey-Stolle
M Fernanda
MF
Yuste
Mercedes
M
Carrasco
Carolina
C
Bailly
Christian
C
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D020552:Comet Assay; D004247:DNA / Q000737:chemistry*; D004249:DNA Damage; D006801:Humans; D007364:Intercalating Agents / Q000138:chemical synthesis / Q000494:pharmacology; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors
D000970:Antineoplastic Agents; D007364:Intercalating Agents; D009281:Naphthalenes; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; D004247:DNA