THERAPEUTIC G-QUADRUPLEX LIGANDS

摘要

The invention provides compounds of formula (I): wherein Ar<SUP>1</SUP> 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 C<SUB>1-7</SUB> alkyl, optionally substituted C<SUB>3-20</SUB> heterocyclyl, optionally substituted C<SUB>5-20</SUB> aryl, halo, amino, hydroxy, ether, thio, thioet her, carboxy or cyano; L<SUP>1</SUP> and L<SUP>2 </SUP>are each independently selected from NR <SUP>3</SUP>, C<SUB>2</SUB>H<SUB>2</SUB>, CH<SUB>2</SUB>, -O-, -S- and a bond; Ar<SUP>2</SUP> and Ar<SUP>3</SUP> are independently optionally substituted C <SUB>5</SUB> or C<SUB>6</SUB> aryl or heteroaryl; n is an integer from 1 to 5; R<SUP>1</SUP> and R<SUP>2</SUP> are independently hydrog en, C<SUB>1-7</SUB> alkyl, C<SUB>3-20</SUB> heterocyclyl, or C <SUB>5-20</SUB> aryl, or R<SUP>1</SUP> and R<SUP>2</SUP>, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; R<SUP>3</SUP> is H or C <SUB>1-7</SUB> alkyl; and provided that at least one of Ar <SUP>1</SUP>, Ar<SUP>2</SUP> and Ar<SUP>3</SUP> 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.