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. Author manuscript; available in PMC: 2017 Sep 23.
Published in final edited form as: Chem Rev. 2015 Nov 9;115(22):12546–12629. doi: 10.1021/acs.chemrev.5b00434

Table 30.

Examples of dipeptide caspase -3 inhibitors with various P3 substituents.304

graphic file with name nihms905431t177.jpg enzyme assays IC50, μM
Casp-3		 50% cell protection, nM
PhCH2O- (MX1013) 274 30 250
CH3- 306 250 -
CH3CH2- 307 81 -
PhCH2- 308 61 -
CH3O- 309 37 500
PhCH2CH2- 310 98 -
Isopropyl-O- 311 35 -
CyclopentylCH2O- 312 30 300
PhCH2CH2O- 313 110 -
PhCH2CH2CH2O- 314 46 -
2-Cl-PhCH2O- 315 36 -
3-Cl-PhCH2O- 316 36 -
4-Cl-PhCH2O- 317 34 -
2-F-PhCH2O- 318 38 -
3-F-PhCH2O- 319 29 -
4-F-PhCH2O- 320 28 150
2,4-di-Cl-PhCH2O- (MX1122) 275 25 100
3,4-di-Cl-PhCH2O- 321 21 150
2,5-di-Cl-PhCH2O- 322 15 100
2,4-di-F-PhCH2O- 323 35 -