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

University of Strathclyde

Research output: Contribution to journal › Article › peer-review

14 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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Access to Document

10.1016/j.bmcl.2016.06.040Licence: Unspecified

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

Cite this

@article{13f46a7591564d4881ec72388f542e5d,

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 = "Anti-cancer, Lung cancer, Minor Groove Binders",

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.\}",

year = "2016",

month = aug,

day = "1",

doi = "10.1016/j.bmcl.2016.06.040",

language = "English",

volume = "26",

pages = "3478--3486",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "15",

}

TY - JOUR

T1 - An evaluation of Minor Groove Binders as anti-lung cancer therapeutics

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

Y1 - 2016/8/1

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

UR - https://www.scopus.com/pages/publications/84977575344

UR - https://www.journals.elsevier.com/bioorganic-and-medicinal-chemistry-letters

U2 - 10.1016/j.bmcl.2016.06.040

DO - 10.1016/j.bmcl.2016.06.040

M3 - Article

C2 - 27349332

AN - SCOPUS:84977575344

SN - 0960-894X

VL - 26

SP - 3478

EP - 3486

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 15

ER -

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

Abstract

UN SDGs

Access to Document

Other files and links

Fingerprint

Cite this