Cancer Research Technology Limited

Pharminxo Limited

Tracey Dawn Poole

Andrew David Westwell

Geoffrey Wells

Malcolm Francis Graham Stevens

Malcolm F G Stevens

Ian P Hutchinson

Jane Marie Berry

Malcolm Francis G Stevens

Mei-Sze Chua

A compound of general structure I, wherein the compound is optionally in the form of an N-oxide or S-oxide or prodrug form and/or pharmaceutically acceptable salt thereof wherein:

2-arylbenzothiazole derivatives

This invention pertains to certain 4-(1-(sulfonyl)-1H-indol-2-yl)-4-(hydroxy)-cyclohexa-2,5-dienone compounds, and analogs thereof, including compounds of the following formula, which are, inter alia, antiproliferative agents, anticancer agents, and/or thioredoxin/thioredoxin reductase inhibitors: formula (I) wherein: Ar is a 1-(sulfonyl)-1H-indol-2-yl group; the bond marked &#x3b1; is independently: (a) a single bond; or: (b) a double bond; the bond marked &#x3b2; is independently: (a) a single bond; or: (b) a double bond; the group &#x2014;ORis independently: (a) &#x2014;OH; (b) an ether group (e.g., &#x2014;OMe); or: (c) an acyloxy (i.e., reverse ester) group (e.g., &#x2014;OC(&#x2550;O)Me); each of R, R, R, and R, is independently a ring substituent and is: (a) H; (b) a monovalent monodentate substituent; or: (c) a ring substituent which, together with an adjacent ring substituent, and together with the ring atoms to which these ring substituents are attached, form a fused ring; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. 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, for example, in the treatment of proliferative conditions, (e.g., cancer), and/or conditions mediated by thioredoxin/thioredoxin reductase.

4-(1-(sulfonyl)-1h-indol-2-yl)-4-(hydroxy)-cyclohexa-2,5-dienone compounds and analogs thereof as therapeutic agents

The present invention pertains to compounds of the formula (1) which are, inter alia, antiproliferative agents, anticancer agents, antimycobacterial agents, antituberculosis agents, and/or thioredoxin/thioredoxin reductase inhibitor: wherein: Q is &#x2550;O or &#x2550;N&#x2014;S(&#x2550;O)&#x2014;R;Ris &#x2014;II or optionally substituted Calkyl, Cheterocyclyl, or Caryl; Ar is optionally substituted Caryl; Ris an oxy substituent; the bond marked &#x3b1; is a single bond or a double bond; the bond marked &#x3b2; is a single bond or a double bond; Rand Rare each independently ring substituents; Rand Rare each independently ring substituents; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. 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, for example, in the treatment of proliferative conditions, (e.g., cancer), mycobacterial infections (e.g., tuberculosis), and/or conditions mediated by thioredoxin/thioredoxin reductase 

4-aryl quinols and analogs thereof as therapeutic agents

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.

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Chesterfield, United Kingdom

Tracey Dawn Poole