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

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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.
Original languageEnglish
Number of pages11
JournalBioorganic and Medicinal Chemistry Letters
DOIs
Publication statusAccepted/In press - 15 Jun 2016

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Keywords

  • minor groove binders
  • anti-cancer
  • lung cancer

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