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Minor groove binders substituted by lipophilic groups

Suckling, C.J. and Waigh, R.D. and Khalaf, A.L. and Parkinson, J. and Hunter, I.S. (2003) Minor groove binders substituted by lipophilic groups. In: 19th International Congress on Heterocyclic Chemistry. Elsevier, p. 98. ISBN 0-080443-04-4

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The search for novel anti-infective and anticancer drugs ranges over many types of compound. Following earlier work into the synthesis of compounds that bind into the minor groove of DNA (based upon the well-known N-methylpyrrole amino acid monomer), we have extended our studies to develop compounds including a wide range of alternative heterocyclic rings and alkyl substituents (with Professor Roger Waigh, Pharmaceutical Sciences). [see references] For reasons of commercial significance, the detailed structures of these compounds cannot be disclosed until early 2003 but Scheme2 is illustrative. However we have been gratified to find that some of our compounds containing novel structural features have antibacterial activity against such key organisms as MRSA and Cryptosporidium as well as against a number of fungi including Aspergillus and Candida. Moreover, nmr studies have given us strong insight into the detailed binding of our compounds with DNA. The chief synthetic chemical problems to be solved relate to the efficient solid phase synthesis of compounds containing the new heterocyclic monomers and, in some cases, to the monomers themselves. These problems are being addressed in partnership with LINK Technologies, a local biotech company, through the Teaching Company Scheme. There are also major structural and biochemical problems to be tackled. Some of our active compounds have very potent and specific binding patterns to DNA; in order to make further progress in targeting specific genes, the structural basis for this must be understood. Having discovered significant antibacterial and antifungal activity we are also keen to confirm and extend preliminary results that indicate interference with the action of cytokines in some cell types.