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13
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37549020046
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The phrase "Lead-Oriented Synthesis" was used by Drs Ian Churcher and Alan Nadin at the GSK Novel Synthetic Methods Symposium, GSK Stevenage, 24-25 May 2010. To the authors' knowledge, this is its first use
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T. E. Nielsen S. L. Schreiber Angew. Chem., Int. Ed. 2008 47 48 56
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(2008)
Angew. Chem., Int. Ed.
, vol.47
, pp. 48-56
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Nielsen, T.E.1
Schreiber, S.L.2
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15
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28444498830
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M. A. Koch A. Schuffenhauer M. Scheck S. Wetzel M. Casaulta A. Odermatt P. Ertl H. Waldmann Proc. Natl. Acad. Sci. U. S. A. 2005 102 17272 17277
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(2005)
Proc. Natl. Acad. Sci. U. S. A.
, vol.102
, pp. 17272-17277
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Koch, M.A.1
Schuffenhauer, A.2
Scheck, M.3
Wetzel, S.4
Casaulta, M.5
Odermatt, A.6
Ertl, P.7
Waldmann, H.8
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17
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33746047675
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A. Nören-Müller I. Reis-Corrêa, Jr H. Prinz C. Rosenbaum K. Saxena H. J. Schwalbe D. Vestweber G. Cagna S. Schunk O. Schwarz H. Schiewe H. Waldmann Proc. Natl. Acad. Sci. U. S. A. 2006 103 10606 10611
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(2006)
Proc. Natl. Acad. Sci. U. S. A.
, vol.103
, pp. 10606-10611
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Nören-Müller, A.1
Reis-Corrêa Jr., I.2
Prinz, H.3
Rosenbaum, C.4
Saxena, K.5
Schwalbe, H.J.6
Vestweber, D.7
Cagna, G.8
Schunk, S.9
Schwarz, O.10
Schiewe, H.11
Waldmann, H.12
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19
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78650459806
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For a recent example, see
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P. A. Clemons N. E. Bodycombe H. A. Carrinski J. A. Wilson A. F. Shamji B. K. Wagner A. N. Koehler S. L. Schreiber Proc. Natl. Acad. Sci. U. S. A. 2010 107 18787 18792
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(2010)
Proc. Natl. Acad. Sci. U. S. A.
, vol.107
, pp. 18787-18792
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Clemons, P.A.1
Bodycombe, N.E.2
Carrinski, H.A.3
Wilson, J.A.4
Shamji, A.F.5
Wagner, B.K.6
Koehler, A.N.7
Schreiber, S.L.8
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26
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65949097509
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We chose these cell lines as similar spirocyclic piperidines were shown to be active in THP-1 assays by Itoh et al
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A. F. Newton S. J. Roe J.-C. Legeay P. Aggarwal C. Gignoux N. J. Birch R. Nixon M.-L. Alcaraz R. A. Stockman Org. Biomol. Chem. 2009 7 2274 2277
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(2009)
Org. Biomol. Chem.
, vol.7
, pp. 2274-2277
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Newton, A.F.1
Roe, S.J.2
Legeay, J.-C.3
Aggarwal, P.4
Gignoux, C.5
Birch, N.J.6
Nixon, R.7
Alcaraz, M.-L.8
Stockman, R.A.9
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27
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0037136021
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Itoh et al. 27 also found compounds with silyl groups gave the highest activity in their THP-1 assays. This may be down to better cell membrane permeation of these more lipophilic compounds, although the inactivity of 18 in the A549 cell lines rules out any generic cytotoxicity effect associated with lipophilic molecules
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M. Itoh J. Kuwahara K. Itoh Y. Fukuka M. Kohya M. Shindo K. Shishido Bioorg. Med. Chem. Lett. 2002 12 2069
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(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 2069
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Itoh, M.1
Kuwahara, J.2
Itoh, K.3
Fukuka, Y.4
Kohya, M.5
Shindo, M.6
Shishido, K.7
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