1262546-35-9Relevant academic research and scientific papers
A novel series of G-quadruplex ligands with selectivity for HIF-expressing osteosarcoma and renal cancer cell lines
Lombardo, Caterina M.,Welsh, Sarah J.,Strauss, Sandra J.,Dale, Aaron G.,Todd, Alan K.,Nanjunda, Rupesh,Wilson, W. David,Neidle, Stephen
, p. 5984 - 5988 (2012/11/07)
A series of naphthalene derivatives with disubstituted triazole side-arms have been assembled by click chemistry. Lead compounds show a high level of selectivity for renal, osteo- and Ewing's sarcomas that express the HIF-1α transcription factor. They also interact selectively with the quadruplex DNAs located in the promoter of the HIF genes and it is suggested that the mechanism of action involves inhibition of transcription by drug-mediated quadruplex stabilization in these regions.
Structure-based design of selective high-affinity telomeric quadruplex-binding ligands
Lombardo, Caterina Maria,Martinez, Iria Sanchez,Haider, Shozeb,Gabelica, Valerie,De Pauw, Edwin,Moses, John E.,Neidle, Stephen
, p. 9116 - 9118 (2011/02/23)
A library of triazole-based telomeric quadruplex-selective ligands has been developed that mimic an established family of tri-substituted acridine-based ligands, using crystal structure data as a starting-point for computer-based design. Binding affinities, estimated by electrospray mass spectrometry, are in accord with the design concept.
