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

Fraser J. Scott, Mireia Puig-Sellart, Abedawn I. Khalaf, Catherine J. Henderson, Gareth Westrop, David G. Watson, Katharine Carter, M. Helen Grant, Colin J. Suckling

Research output: Contribution to journalArticle

8 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)3478-3486
Number of pages9
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number15
Early online date16 Jun 2016
DOIs
Publication statusPublished - 1 Aug 2016
Externally publishedYes

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