TY - JOUR
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
N1 - © 2016 Elsevier Ltd. All rights reserved.
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, An evaluation of Minor Groove Binders as anti-lung cancer therapeutics, Bioorganic & Medicinal Chemistry Letters,
Volume 26, Issue 15, 2016, Pages 3478-3486, https://doi.org/10.1016/j.bmcl.2016.06.040
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 - 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
SN - 0960-894X
VL - 26
SP - 3478
EP - 3486
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 15
ER -