921201-93-6Relevant articles and documents
Click chemistry assembly of G-quadruplex ligands incorporating a diarylurea scaffold and triazole linkers
Drewe, William C.,Neidle, Stephen
supporting information; experimental part, p. 5295 - 5297 (2009/03/11)
A series of diarylurea ligands were designed to interact selectively with G-quadruplexes and were synthesised using copper(I) catalysed 'click' chemistry to incorporate the 1,4-substituted 1,2,3-triazole ring into the core of the ligands; the optimal ligands demonstrate a high degree of selective telomeric G-quadruplex stabilisation and are not cytotoxic in several cancer cell lines. The Royal Society of Chemistry.
THERAPEUTIC G-QUADRUPLEX LIGANDS
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Page/Page column 23, (2008/12/05)
The invention provides compounds of formula (I): wherein Ar1 is a monocyclic aryl or heteroaryl; X and Y are each independe ntly a group of formula (II): Z is absent, a group of formula (II), optionally substituted C1-7 alkyl, optionally substituted C3-20 heterocyclyl, optionally substituted C5-20 aryl, halo, amino, hydroxy, ether, thio, thioet her, carboxy or cyano; L1 and L2 are each independently selected from NR 3, C2H2, CH2, -O-, -S- and a bond; Ar2 and Ar3 are independently optionally substituted C 5 or C6 aryl or heteroaryl; n is an integer from 1 to 5; R1 and R2 are independently hydrog en, C1-7 alkyl, C3-20 heterocyclyl, or C 5-20 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 C 1-7 alkyl; and provided that at least one of Ar 1, Ar2 and Ar3 is oxazole, triazole or tetrazole. These compounds are thought to bind G -quadruplexes formed in human telomeres and are therefore useful in anti -cancer therapy. The invention also provides pharmaceutical compositions comprising the novel compounds, and methods for their manufacture.
