| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1368498 | Bioorganic & Medicinal Chemistry Letters | 2016 | 9 Pages |
•Minor Groove Binders (MGBs) possess activity against the melanoma cancer cell line B16-F10.•5 MGBs have been identified that have IC50s less than that of a standard therapy, Gemcitabine.•Lead compound around >70 more active than Gemcitabine and a favourable selectivity index of >125.
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.
Graphical abstractA distamycin derived minor groove binder with superior in vitro anti-lung cancer activity to Gemcitabine.Figure optionsDownload full-size imageDownload as PowerPoint slide
