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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 28.

Examples of dipeptide caspases inhibitors with various N-capping substituents occupying P3 position.

graphic file with name nihms905431t162.jpg enzyme assays IC50, μM
mCasp-1 Casp-3 Casp-6 Casp-7 Casp-8 Ref
Ac-DEVD-CHO 83 0.05 0.0035 0.01 0.01 0.08 275
1-Naphthyloxy acetyl 277 0.570 0.135 0.940 1.81 0.770
2- Naphthyloxy acetyl 278 10 0.944 18.56 8.87 > 10
2-(1-Naphthyloxy)propionyl 279 3.99 0.376 1.28 1.32 2.43
1-Naphthylmercapto acetyl 280 2.75 0.195 1.43 1.74 7.42
3-(1-Naphthyloxy)propionyl 281 0.686 0.059 0.305 1.37 9.81
4-Methoxy-1-naphthyloxy acetyl 282 0.831 0.263 22.6 4.08 1.45
4-Chloro-1-naphthyloxy acetyl 283 0.429 0.231 12.0 3.38 1.69
2,4-Dichloro-1-naphthyloxy acetyl 284 0.141 0.357 21.4 3.61 3.04
2-Biphenoxy acetyl 285 0.636 0.095 0.717 2.02 1.71
(2-Cyclopentyl)phenoxy acetyl 286 0.538 0.197 3.37 1.49 1.86
graphic file with name nihms905431t163.jpg enzyme assays IC50, μM Cell assay IC50, μM
Casp-1 Casp-3 Casp-7 Casp-8 NT2 cells Ref
Ac-DEVD-CHO 83 0.19 0.027 0.087 0.13 > 100 306
2,5-di-(OCH3)-Ph-CH2- 287 6.0 0.048 3.2 6.6 10
2,4-di-Br-Ph-CH2- 288 0.86 0.14 1.5 8.7 63.0
5-fluoro-1H-indole- 289 2.6 0.083 1.4 3.3 55.0
2-CH3O-Ph-CH2- 290 28 0.31 2.7 15.5 -
3-CH3O-Ph-CH2- 291 14 0.21 3.1 14 60.0
Ph-CH2- 292 22 0.75 8.4 22.5 -
2-CH3O-4-Br-Ph-CH2- 293 3.1 0.06 3.1 2.3 9.0
2-CH3O-4-acetyl-Ph-CH2- 294 5.9 0.01 0.13 2.9 2.0