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

Fraser J. Scott, Mireia Puig-Sellart, Abedawn I. Khalaf, Catherine J. Henderson, Gareth Westrop, David G. Watson, Katharine Carter, M. Helen Grant, Colin J. Suckling

Research output: Contribution to journalArticle

7 Citations (Scopus)

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
Pages (from-to)3478-3486
Number of pages9
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number15
Early online date16 Jun 2016
DOIs
Publication statusPublished - 1 Aug 2016
Externally publishedYes

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gemcitabine
Binders
Lung Neoplasms
Biological Products
Early Detection of Cancer
Melanoma
Screening
Cells
Cell Line
Therapeutics
Neoplasms

Cite this

Scott, F. J., Puig-Sellart, M., Khalaf, A. I., Henderson, C. J., Westrop, G., Watson, D. G., ... Suckling, C. J. (2016). An evaluation of Minor Groove Binders as anti-lung cancer therapeutics. Bioorganic and Medicinal Chemistry Letters, 26(15), 3478-3486. https://doi.org/10.1016/j.bmcl.2016.06.040
Scott, Fraser J. ; Puig-Sellart, Mireia ; Khalaf, Abedawn I. ; Henderson, Catherine J. ; Westrop, Gareth ; Watson, David G. ; Carter, Katharine ; Grant, M. Helen ; Suckling, Colin J. / An evaluation of Minor Groove Binders as anti-lung cancer therapeutics. In: Bioorganic and Medicinal Chemistry Letters. 2016 ; Vol. 26, No. 15. pp. 3478-3486.
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Scott, FJ, Puig-Sellart, M, Khalaf, AI, Henderson, CJ, Westrop, G, Watson, DG, Carter, K, Grant, MH & Suckling, CJ 2016, 'An evaluation of Minor Groove Binders as anti-lung cancer therapeutics', Bioorganic and Medicinal Chemistry Letters, vol. 26, no. 15, pp. 3478-3486. https://doi.org/10.1016/j.bmcl.2016.06.040

An evaluation of Minor Groove Binders as anti-lung cancer therapeutics. / Scott, Fraser J.; Puig-Sellart, Mireia; Khalaf, Abedawn I.; Henderson, Catherine J.; Westrop, Gareth; Watson, David G.; Carter, Katharine; Grant, M. Helen; Suckling, Colin J.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 26, No. 15, 01.08.2016, p. 3478-3486.

Research output: Contribution to journalArticle

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Scott FJ, Puig-Sellart M, Khalaf AI, Henderson CJ, Westrop G, Watson DG et al. An evaluation of Minor Groove Binders as anti-lung cancer therapeutics. Bioorganic and Medicinal Chemistry Letters. 2016 Aug 1;26(15):3478-3486. https://doi.org/10.1016/j.bmcl.2016.06.040