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

  • Bioorg Med Chem Lett. 2016 Aug 1;26(15):3478-86. doi: 10.1016/j.bmcl.2016.06.040.
Fraser J Scott  1 ,  Mireia Puig-Sellart  2 ,  Abedawn I Khalaf  1 ,  Catherine J Henderson  3 ,  Gareth Westrop  2 ,  David G Watson  2 ,  Katharine Carter  2 ,  M Helen Grant  3 ,  Colin J Suckling  1
Affiliations
  • 1. WestCHEM, Department of Pure and Applied Chemistry, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom.
  • 2. Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, 161 Cathedral Street, Glasgow G4 0RE, United Kingdom.
  • 3. Department of Biomedical Engineering, University of Strathclyde, Wolfson Centre, Glasgow G1 0NW, United Kingdom.
PMID: 27349332 DOI: 10.1016/j.bmcl.2016.06.040
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
Anti-cancer; Lung cancer; Minor Groove Binders.
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