An evaluation of minor groove binders as anti-lung cancer therapeutics

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6 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.
LanguageEnglish
Number of pages11
JournalBioorganic and Medicinal Chemistry Letters
DOIs
Publication statusAccepted/In press - 15 Jun 2016

Fingerprint

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

Keywords

  • minor groove binders
  • anti-cancer
  • lung cancer

Cite this

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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.",
keywords = "minor groove binders, anti-cancer, lung cancer",
author = "Fraser Scott and Abedawn Khalaf and Colin Suckling and Katharine Carter and Mary Grant and Catherine Henderson and Gareth Westrop and David Watson",
year = "2016",
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day = "15",
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T1 - An evaluation of minor groove binders as anti-lung cancer therapeutics

AU - Scott, Fraser

AU - Khalaf, Abedawn

AU - Suckling, Colin

AU - Carter, Katharine

AU - Grant, Mary

AU - Henderson, Catherine

AU - Westrop, Gareth

AU - Watson, David

PY - 2016/6/15

Y1 - 2016/6/15

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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 - minor groove binders

KW - anti-cancer

KW - lung cancer

U2 - 10.1016/j.bmcl.2016.06.040

DO - 10.1016/j.bmcl.2016.06.040

M3 - Article

JO - Bioorganic and Medicinal Chemistry Letters

T2 - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

ER -