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

doi:10.1016/j.bmcl.2016.06.040

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 journal › Article › peer-review

12 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 language	English
Pages (from-to)	3478-3486
Number of pages	9
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	26
Issue number	15
Early online date	16 Jun 2016
DOIs	https://doi.org/10.1016/j.bmcl.2016.06.040
Publication status	Published - 1 Aug 2016
Externally published	Yes

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https://pure.strath.ac.uk/portal/en/publications/an-evaluation-of-minor-groove-binders-as-antilung-cancer-therapeutics(4783a4d8-0a11-4cc2-a2b4-ba3d8ea5fa1f).htmlLicence: CC BY-NC-ND

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title = "An evaluation of Minor Groove Binders as anti-lung cancer therapeutics",

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.",

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

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AU - Scott, Fraser J.

AU - Puig-Sellart, Mireia

AU - Khalaf, Abedawn I.

AU - Henderson, Catherine J.

AU - Westrop, Gareth

AU - Watson, David G.

AU - Carter, Katharine

AU - Grant, M. Helen

AU - Suckling, Colin J.

PY - 2016/8/1

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N2 - 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.

AB - 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.

KW - Anti-cancer

KW - Lung cancer

KW - Minor Groove Binders

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SN - 0960-894X

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

Abstract

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