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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 25.

Examples of dipeptide caspases inhibitors based on 1-Naphthyl-CO-Val-Asp-scaffold with various leaving groups.

graphic file with name nihms905431t153.jpg enzyme assays k3/Ki, M−1s−1 cellular assays IC50, μM Ref
mCasp-1 Casp-3 Casp-6 Casp-8 Con A Monocyte Jurkat
-F 246 129000 207000 36842 71667 3.05 0.95 0.24 274
-OPh 247 3630 19152 2399 4258 38.00 11.17 13.95
-OCO(2,6-Cl2-Ph) 248 52109 725222 56883 17010 2.15 11.50 10.61
-O(1-Naphthylyl) 249 354241 1958905 0 0 2.65 19 > 100
-O(2-Naphthylyl) 250 263 7521 0 0 > 50 15.90 > 100
-O(2,6-F2-Ph) 251 53875 200052 9979 9075 2.40 > 100 2.04
-O(2,3,6-F3-Ph) 252 47081 187700 81749 16972 2.433 - 1.195
-O(2,3,5,6-F4-Ph) 253 77528 267953 78887 30173 2.17 6.25 4.50
-O(2,6-Cl2-Ph) 254 25259 178629 87715 2713 2.75 15.32 3.00
graphic file with name nihms905431t154.jpg 255 7572 71138 23909 2266 n.d. n.d. 28 297
graphic file with name nihms905431t155.jpg 256 9396 35478 509 295 n.d. n.d. 46
graphic file with name nihms905431t156.jpg 257 42463 143850 5804 6344 n.d. n.d. 71
graphic file with name nihms905431t157.jpg 258 1191 38119 975 3059 n.d. n.d. 102
graphic file with name nihms905431t158.jpg 259 24834 113766 5147 3199 n.d. n.d. 37
graphic file with name nihms905431t159.jpg 260 45379 168736 44007 18230 n.d. n.d. 137