An evaluation of Minor Groove Binders as anti-lung cancer therapeutics.
Scott FJ, Puig-Sellart M, Khalaf AI, Henderson CJ, Westrop G, Watson DG, Carter K, Grant MH, Suckling CJ.
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.