An evaluation of Minor Groove Binders as anti-lung cancer therapeutics

Scott, Fraser J., Puig-Sellart, Mireia, Khalaf, Abedawn I. , Henderson, Catherine J., Westrop, Gareth, Watson, David G., Carter, Katharine, Grant, M. Helen and Suckling, Colin J. (2016) An evaluation of Minor Groove Binders as anti-lung cancer therapeutics. Bioorganic & Medicinal Chemistry Letters, 26 (15). pp. 3478-3486. ISSN 0960-894X

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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.

Keywords:Minor Groove Binders, Anti-cancer, Lung cancer, JCNotOpen
Subjects:F Physical Sciences > F150 Medicinal Chemistry
Divisions:College of Science > School of Chemistry
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ID Code:25564
Deposited On:11 Jan 2017 14:51

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