856047-84-2Relevant academic research and scientific papers
G-QUADRUPLEX STABILISING AGENT
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Page/Page column 18-19, (2012/10/18)
A compound of formula (I) (Formula (I)) wherein Ar1 is a bicyclic aryl or heteroaryl, which may be optionally substituted; X and Y are each independently a group of formula (II): (Formula (II)) L1 and L2 are each independently selected from NR3, C2H2, CH2, -O-, -S- and a bond; Ar2 and Ar3 are independently optionally substituted C5 or C6 aryl or heteroaryl; Q is selected from NH(C=O), NR3, S, O; n is an integer from 1 to 5; R1 and R2 are optionally substituted and are independently hydrogen, C1-7 alkyl, C3-20 heterocyclyl, or C5-20 aryl, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; R3 is H or C1-7 alkyl.
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
supporting information, 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
supporting information; experimental part, 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.
