Scott, Fraser J., Puig-Sellart, Mireia, Khalaf, Abedawn I. et al, 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
Full content URL: https://www.sciencedirect.com/science/article/pii/...
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Item Type: | Article |
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Item Status: | Live Archive |
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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.
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