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. Author manuscript; available in PMC: 2016 Feb 16.
Published in final edited form as: J Med Chem. 2011 Jun 7;54(13):4678–4693. doi: 10.1021/jm2003427

Table 3.

Antiproliferative Activity of Modified Compounds with Improved Aqueous Solubility

graphic file with name nihms753533t3.jpg
IC50 ± SEM (µM)
apart B16-F1 A375 DU 145 PC-3 LNCaP PPC-1
28 4-OTBDMSPh 0.5 ± 0.2 0.7 ± 0.3 0.434 ± 0.030 0.183 ± 0.024 0.549 0.246 ± 0.008
29 4-OHPh 0.11 ± 0.02 0.10 ± 0.01 0.116 ± 0.014 0.087 ± 0.005 0.103 ± 0.009 0.076 ± 0.002
32 2-indolyl 0.043 ± 0.021 0.019 ± 0.009 0.032 ± 0.001 0.024 ± 0.004 0.028 ± 0.003 0.028 ± 0.002
36 5-indolyl 0.025 ± 0.013 0.008 ± 0.001 0.013 ± 0.001 0.007 ± 0.001 0.010 ± 0.001 0.008 ± 0.001
38 4-BocNHCH2Ph 2.9 ± 0.4 7.9 ± 0.5 4.3 ± 3.7 3.1 ± 1.7 2.6 ± 0.9 2.7 ± 1.5
39 4-NH2CH2Ph 0.038 ± 0.011 0.041 ± 0.013 0.025 ± 0.001 0.080 ± 0.007 0.013 ± 0.001 0.034 ± 0.001
40 4-NHMeCH2Ph >10 >10 ~10 >10 1.14 ± 0.08 ~10
42 4-NMe2CH2Ph >10 >10 >10 >10 1.025 ± 0.2 >10
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