| 16302795 |
Falgueyret JP, Desmarais S, Oballa R, Black WC, Cromlish W, Khougaz K, Lamontagne S, Masse F, Riendeau D, Toulmond S, Percival MD: Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J Med Chem. 2005 Dec 1;48(24):7535-43.
The aryl-piperazine-containing cathepsin K inhibitor CRA-013783/L-006235 (1) displays greater than 4000-fold selectivity against the lysosomal/endosomal antitargets cathepsin B, L, and S. |
35(0,1,1,5) |
Details |
| 12662032 |
Chen CY, Dagneau P, Grabowski EJ, Oballa R, O'Shea P, Prasit P, Robichaud J, Tillyer R, Wang X: Practical asymmetric synthesis of a potent Cathepsin K inhibitor. J Org Chem. 2003 Apr 4;68(7):2633-8.
The final step of the convergent synthesis of 1 was completed via Suzuki coupling of aryl bromide 7a with unprotected aryl piperazine boronic acid 13. |
2(0,0,0,2) |
Details |