TY - JOUR
T1 - An evaluation of minor groove binders as anti-Trypanosoma brucei brucei therapeutics
AU - Scott, Fraser J.
AU - Khalaf, Abedawn I.
AU - Giordani, Federica
AU - Wong, Pui Ee
AU - Duffy, Sandra
AU - Barrett, Michael
AU - Avery, Vicky M.
AU - Suckling, Colin J.
PY - 2016/6/30
Y1 - 2016/6/30
N2 - A series of 32 structurally diverse MGBs, derived from the natural product distamycin, was evaluated for activity against Trypanosoma brucei brucei. Four compounds have been found to possess significant activity, in the nanomolar range, and represent hits for further optimisation towards novel treatments for Human and Animal African Trypanosomiases. Moreover, SAR indicates that the head group linking moiety is a significant modulator of biological activity.
AB - A series of 32 structurally diverse MGBs, derived from the natural product distamycin, was evaluated for activity against Trypanosoma brucei brucei. Four compounds have been found to possess significant activity, in the nanomolar range, and represent hits for further optimisation towards novel treatments for Human and Animal African Trypanosomiases. Moreover, SAR indicates that the head group linking moiety is a significant modulator of biological activity.
KW - minor groove binders
KW - antiparasitic activity
KW - african trypanosmiasis
UR - http://www.sciencedirect.com/science/article/pii/S0223523416302471
U2 - 10.1016/j.ejmech.2016.03.064
DO - 10.1016/j.ejmech.2016.03.064
M3 - Article
SN - 0223-5234
VL - 116
SP - 116
EP - 125
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -