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. Author manuscript; available in PMC: 2019 Sep 26.
Published in final edited form as: Mol Pharm. 2019 Jun 19;16(7):3065–3071. doi: 10.1021/acs.molpharmaceut.9b00293

Table 1.

In vitro metabolic stability in mouse liver microsome of PTM and PTM-inspired thioether-analogues.

Entry R T1/2 (min) Intrinsic Clearance (μL/min/mg) Entry R T1/2 (min) Intrinsic Clearance (μL/min/mg)
Sunitinib - 13.1 53 2j 3-CF3C6H4 3.2 217
PTM - 13.6 51 2k 2-CF3C6H4 5.7 122
2a Ph 1.4 495 2l 4-NO2C6H4 1.5 462
2b 4-ClC6H4 1.6 433 2m 3,5-diFC6H4 1.6 433
2c 4-MeOC6H4 1.3 533 2n 3,5-diCF3C6H4 7.4 94
2d 4-MeC6H4 1.4 495 2o -thiophene 1.6 433
2e 4-FC6H4 2.8 248 2p -naphthyl 1.7 408
2f 3-FC6H4 1.6 433 2q -CH3 9.5 73
2g 2-FC6H4 1.8 385 2r 4-FBn 1.4 495
2h 4-BrC6H4 1.5 462 2s 4-CH3C6H4 10.4 67
2i 4-CF3C6H4 1.6 433 2t -CH2CH3 15.0 46