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Citation

BibTex format

@article{Rueda-Zubiaurre:2020:10.1021/acs.jmedchem.9b00898,
author = {Rueda-Zubiaurre, A and Yahiya, S and Fischer, O and Hu, X and Saunders, C and Sharma, S and Straschil, U and Shen, J and Tate, EW and Delves, M and Baum, J and Barnard, A and Fuchter, MJ},
doi = {10.1021/acs.jmedchem.9b00898},
journal = {Journal of Medicinal Chemistry},
pages = {2240--2262},
title = {Structure-activity relationship studies of a novel class of transmission blocking antimalarials targeting male gametes.},
url = {http://dx.doi.org/10.1021/acs.jmedchem.9b00898},
volume = {63},
year = {2020}
}
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RIS format (EndNote, RefMan)

TY  - JOUR
AB  - Malaria is still a leading cause of mortality among children in the developing world, and despite the immense progress made in reducing the global burden, further efforts are needed if eradication is to be achieved. In this context, targeting transmission is widely recognized as a necessary intervention towards that goal. After carrying out a screen to discover new transmission-blocking agents, herein we report our medicinal chemistry efforts to study the potential of the most robust hit, DDD01035881, as a male-gamete targeted compound. We reveal key structural features for the activity of this series and identify analogues with greater potency and improved metabolic stability. We believe this study lays the groundwork for further development of this series as a transmission blocking agent.
AU  - Rueda-Zubiaurre,A
AU  - Yahiya,S
AU  - Fischer,O
AU  - Hu,X
AU  - Saunders,C
AU  - Sharma,S
AU  - Straschil,U
AU  - Shen,J
AU  - Tate,EW
AU  - Delves,M
AU  - Baum,J
AU  - Barnard,A
AU  - Fuchter,MJ
DO  - 10.1021/acs.jmedchem.9b00898
EP  - 2262
PY  - 2020///
SN  - 0022-2623
SP  - 2240
TI  - Structure-activity relationship studies of a novel class of transmission blocking antimalarials targeting male gametes.
T2  - Journal of Medicinal Chemistry
UR  - http://dx.doi.org/10.1021/acs.jmedchem.9b00898
UR  - https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b00898
UR  - http://hdl.handle.net/10044/1/73275
VL  - 63
ER  -
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Contact

Prof. Ed Tate
GSK Chair in Chemical Biology
Department of Chemistry
Molecular Sciences Research Hub, White City Campus,
82 Wood Lane, London, W12 0BZ

e.tate@imperial.ac.uk
Tel: +44 (0)20 759 + ext 43752 or 45821