2. Academic Validation
  3. An evaluation of Minor Groove Binders as anti-lung cancer therapeutics

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

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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