Selective G-quadruplex ligands: the significant role of side chain charge density in a series of perylene derivatives.
The human telomeric G-quadruplex structure is a promising target for the design of cancer drugs. The selectivity of G-quadruplex ligands with respect to duplex genomic DNA is of especial importance. The high selectivity of polyamine conjugated perylene derivatives appears to be regulated by side-chain charge density, as indicated by data from a FRET melting assay and induced CD spectroscopy.
Dipartimento di Chimica, Sapienza Università di Roma, Roma, Italy.
Emanuela
E
Micheli
Caterina Maria
CM
Lombardo
Danilo
D
D'Ambrosio
Marco
M
Franceschin
Stephen
S
Neidle
Maria
M
Savino
D000970:Antineoplastic Agents / Q000737:chemistry*; D002942:Circular Dichroism; D031541:Fluorescence Resonance Energy Transfer; D054856:G-Quadruplexes; D006801:Humans; D008024:Ligands; D010569:Perylene / Q000737:chemistry*; D011073:Polyamines / Q000737:chemistry; D019098:Telomerase / Q000037:antagonists & inhibitors / Q000378:metabolism; D016615:Telomere / Q000737:chemistry
D000970:Antineoplastic Agents; D008024:Ligands; D011073:Polyamines; D010569:Perylene; D019098:Telomerase