TY - JOUR
T1 - Synthesis and evaluation of 9,9-dimethylxanthene tricyclics against trypanothione reductase, Trypanosoma brucei, Trypanosoma cruzi and Leishmania donovani
AU - Chibale, Kelly
AU - Visser, Mark
AU - Yardley, Vanessa
AU - Croft, Simon L.
AU - Fairlamb, Alan H.
N1 - Funding Information:
We thank Ahilan Saravanamuthu and Dr. David Parkin for help with enzyme assays, Peter J. Rock and Diane Rowland for help with the antiparasitic in vitro assays. Financial support from the Wellcome Trust (International Research Development grant to KC, grant no. 052075/Z/97). Additional support from the University of Cape Town and Foundation for Research Development (KC) is gratefully acknowledged. This investigation received financial support from the UNDP/World Bank/WHO Special Programme for Research and Training in Tropical Diseases (TDR) (SLC and VY). AHF is supported by the Wellcome Trust.
PY - 2000/6/5
Y1 - 2000/6/5
N2 - Derivatives of 9,9-dimethylxanthene was synthesised and evaluated against trypanothione reductase (TR) and in vitro against parasitic trypanosomes and leishmania. High in vitro antiparasitic activity was observed for some derivatives with one compound showing high activity against all three parasites (ED50 values of 0.02, 0.48 and 0.32 μM, for Trypanosoma brucei, Trypanosoma cruzi, and Leishmania donovani, respectively). The lack of correlation between inhibitory activity against TR and ED50 values suggests that TR is not the target. (C) 2000 Elsevier Science Ltd. All rights reserved.
AB - Derivatives of 9,9-dimethylxanthene was synthesised and evaluated against trypanothione reductase (TR) and in vitro against parasitic trypanosomes and leishmania. High in vitro antiparasitic activity was observed for some derivatives with one compound showing high activity against all three parasites (ED50 values of 0.02, 0.48 and 0.32 μM, for Trypanosoma brucei, Trypanosoma cruzi, and Leishmania donovani, respectively). The lack of correlation between inhibitory activity against TR and ED50 values suggests that TR is not the target. (C) 2000 Elsevier Science Ltd. All rights reserved.
UR - http://www.scopus.com/inward/record.url?scp=0034608699&partnerID=8YFLogxK
U2 - 10.1016/S0960-894X(00)00154-2
DO - 10.1016/S0960-894X(00)00154-2
M3 - Article
C2 - 10866368
AN - SCOPUS:0034608699
SN - 0960-894X
VL - 10
SP - 1147
EP - 1150
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 11
ER -