e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors
…, SK Davidsen, PA Marcotte, I Elmore, DH Albert…
Index: Sheppard, George S.; Florjancic, Alan S.; Giesler, Jamie R.; Xu, Lianhong; Guo, Yan; Davidsen, Steven K.; Marcotte, Patrick A.; Elmore, Ildiko; Albert, Daniel H.; Magoc, Terrance J.; Bouska, Jennifer J.; Goodfellow, Carole L.; Morgan, Douglas W.; Summers, James B. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 22 p. 3251 - 3256
A series of succinyl hydroxamate MMP inhibitors were prepared incorporating an aryl amino ketone moiety in place of the more typical C-terminal amino acid amides. Compounds of the C-terminal ketone series displayed potent inhibition of MMPs. Several compounds of the series were shown to be orally bioavailable.