MED
derSluis, T. Makhnevych, F. J. Vizeacoumar, S. Alizadeh, S. Bahr, R. L.
of an affinity probe has set the stage for biological evaluation
and target identification of trans-11 (“tamoxilog”), the trans
isomer of NSC 670224. Probe synthesis and full biological stud-
ies are ongoing and will be disclosed in due course.
Brost, Y. Chen, M. Cokol, R. Deshpande, Z. Li, Z.-Y. Lin, W. Liang, M. Mar-
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Full details of synthetic protocols are provided in the Supporting
Information. CCDC 862851, 862852, 862853, 862854, 862855 con-
tain the supplementary crystallographic data for this paper. These
data can be obtained free of charge from The Cambridge Crystallo-
Yeast growth assays: Wild-type cells (strain BY4741)[22] were grown
in yeast extract peptone dextrose (YPD) media at 308C. Cells were
counted by using a hemocytometer, and cultures were diluted to
8ꢁ105 cellsmLꢀ1. The desired concentration of tamoxifen, trans-11
(“tamoxilog”) and related compounds (5 mm) or DMSO was added,
and cultures were incubated at 308C with rotation. Optical density
at 600 nm (OD600) was recorded every 1.5–2 h, starting at the time
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Acknowledgements
The authors would like to thank the US National Institutes of
Health for support of this work (5R01GM084530-08 to R.S.L.). In
addition, this research was supported in part by a special re-
search grant awarded by the Committee on Research from the
University of California, Santa Cruz (USA) to G.A.H. Thanks go to
Dr. Allen G. Oliver (Notre Dame University, USA) and the graduate
student crystallographers Dr. David L. Rogow and Honghan Fei
(University of California, Santa Cruz, USA) for solving the X-ray
structures. Single-crystal, X-ray diffraction data were recorded on
an instrument supported by the US National Science Foundation
(Major Research Instrumentation (MRI) program; grant no. CHE-
0521569). The authors would also like to thank Prof. Roger G. Li-
nington (University of California, Santa Cruz, USA) for insightful
NMR discussions as well as LCMS assistance from one of his
graduate students, Laura Sanchez.
[22] C. Baker Brachmann, A. Davies, G. J. Cost, E. Caputo, J. Li, P. Hieter, J. D.
Keywords: affinity probes · drug discovery · high-throughput
screening · medicinal chemistry · tamoxifen
Received: January 18, 2012
[1] M. Costanzo, A. Baryshnikova, J. Bellay, Y. Kim, E. D. Spear, C. S. Sevier, H.
Ding, J. L. Y. Koh, K. Toufighi, S. Mostafavi, J. Prinz, R. P. St. Onge, B. Van-
Published online on February 29, 2012
ChemMedChem 2012, 7, 761 – 765
ꢀ 2012 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
765