59417-11-7Relevant academic research and scientific papers
New Analogues of Amonafide and Elinafide, Containing Aromatic Heterocycles: Synthesis, Antitumor Activity, Molecular Modeling, and DNA Binding Properties
Bra?a, Miguel F.,Cacho, Mónica,García, Mario A.,De Pascual-Teresa, Beatriz,Ramos, Ana,Domínguez, M. Teresa,Pozuelo, José M.,Abradelo, Cristina,Rey-Stolle, María Fernanda,Yuste, Mercedes,Bá?ez-Coronel, Mónica,Lacal, Juan Carlos
, p. 1391 - 1399 (2004)
Amonafide- and elinafide-related mono and bisintercalators, modified by the introduction of a π-excedent furan or thiophene ring fused to the naphthalimide moiety, have been synthesized. These compounds have shown an interesting antitumor profile. The best compound, 9, was 2.5-fold more potent than elinafide against human colon carcinoma cells (HT-29). Molecular dynamic simulations and physicochemical experiments have demonstrated that these compounds are capable of forming stable DNA complexes. These results, together with those previously reported by us for imidazo- and pyrazinonaphthalimide analogues, have prompted us to propose that the DNA binding process does not depend on the electronic nature of the fused heterocycle.
Polycyclic and heterocyclic chromophores for bis-imide tumoricidals
-
, (2008/06/13)
Anticancer compounds of formula I: STR1 and pharmaceutically acceptable salts thereof, wherein: R1, R2 and R3 are independently selected H, CH3, NH2, NO2, and CN; R9 and R10 are H or alkyl or halo, X1 and Y1 or X2 and Y2, when present, join together to form, independently, a six membered 1N heterocycle substituted with 1-2 R3 ; or the group: STR2 wherein one of W or Z is C=O and the other is C=O, NH, S or O; or when X2 and Y2 are not joined together and when R2 is in the 4-position, then X2 and R2 may join together to form an ethylene bridge; are disclosed.
