Cancer Research Technology Limited

Malcolm F G Stevens

Tracey Dawn Poole

Andrew David Westwell

Lloyd Royston Kelland

Robert A Heald

Mei-Sze Chua

Ian P Hutchinson

The present invention pertains to certain N,N-disubstituted quino[4,3,2-kl]acridinium salts of formula (Q) which inhibit telomerase wherein: p is an integer from 0 to 4; q is an integer from 0 to 3; r is an integer from 0 to 4; each Ris &#x2014;H or a ring substituent; each Ris &#x2014;H or a ring substituent; each Ris &#x2014;H or a ring substituent; Ris a nitrogen substituent; Ris a nitrogen substituent; and, Q is an anion. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, and in the treatment of proliferative conditions, such as cancer.

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Substituted 2-phenylbenzazole compounds of formula (I) wherein X represents S or O and Q represents a direct bond, &#x2014;CH2&#x2014; or &#x2014;CH&#x2550;Ch&#x2014;, exhibt selective antiproliferactive activity in respect of mammalian tumour cells. At least in preferred enbodiments the benzene ring of the benzazole nucleus has a halogen substituent, preferably flourine, and the 2-phenyl group has a 4'-amino substituent which may be conjugated with an amino acid to provide a water soluble amino acid amide prodrug or salt thereof.

Substituted 2-arylbenzazole compounds and their use as antitumour agents

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Nottingham, United Kingdom

Malcolm F G Stevens