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Table 1 5-Substituted -cyano(2-oxo-2,3-dihydroindol-3-yl)acetic acid (scaffold A) derivatives with potent AR inhibitory activities

From: QSAR-based rational discovery of novel substituted-4′-iminospiro[indoline-3,3′-[1,2,5]thiadiazolidinyl]-2-one 1′,1′-dioxide with potent in vitro anticancer activity

Compound X R IC50 μM pIC50
I H H 0.85 6.070
II F H 0.28 6.552
III Br H 0.38 6.420
IV NO2 H 1.2 5.920
V H CH2-C6H5 3.2 5.494
VI H CH2-C6H4-P-F 0.57 6.244
VII H CH2-C6H4-P-CF3 0.57 6.244
VIII H CH2-C6H4-P-CH3 0.64 6.193
IX H CH2-C6H4-P-OCH3 0.63 6.200
X F CH3 0.39 6.408
XI F CH2-CH2-Cl 1.34 5.872
XII F CH2-CH2-CH3 0.28 6.552
XIII F CH2-C6H5 0.18 6.744
XIV F CH2-C6H4-P-F 0.13 6.886
XV F CH2-C6H4-P-CF3 0.28 6.552
XVI F CH2-C6H4-P-CH3 0.075 7.124
XVII F CH2-C6H4-P-OCH3 0.11 6.958
XVIII Br CH2-C6H4-P-CH3 0.25 6.602
Sorbinil   0.50 6.301
Fidarestat   0.15 6.823