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An evaluation of minor groove binders as anti-lung cancer therapeutics

Scott, Fraser and Khalaf, Abedawn and Suckling, Colin and Carter, Katharine and Grant, Mary and Henderson, Catherine and Westrop, Gareth and Watson, David (2016) An evaluation of minor groove binders as anti-lung cancer therapeutics. Bioorganic and Medicinal Chemistry Letters. ISSN 0960-894X (In Press)

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Abstract

A series of 47 structurally diverse MGBs, derived from the natural product distamycin, was evaluated for anti-lung cancer activity by screening against the melanoma cancer cell line B16-F10. Five compounds have been found to possess significant activity, more so than a standard therapy, Gemcitabine. Moreover, one compound has been found to have an activity around 70-fold that of Gemcitabine and has a favourable selectivity index of greater than 125. Furthermore, initial studies have revealed this compound to be metabolically stable and thus it represents a lead for further optimisation towards a novel treatment for lung cancer.