220615-34-9Relevant academic research and scientific papers
Biaryl ether retrohydroxamates as potent, long-lived, orally bioavailable MMP inhibitors
Michaelides, Michael R.,Dellaria, Joseph F.,Gong, Jane,Holms, James H.,Bouska, Jennifer J.,Stacey, Jamie,Wada, Carol K.,Heyman,Curtin, Michael L.,Guo, Yan,Goodfellow, Carole L.,Elmore, Ildiko B.,Albert, Daniel H.,Magoc, Terrance J.,Marcotte, Patrick A.,Morgan, Douglas W.,Davidsen, Steven K.
, p. 1553 - 1556 (2001)
A novel series of biaryl ether reverse hydroxamate MMP inhibitors has been developed. These compounds are potent MMP-2 inhibitors with limited activity against MMP-1. Select members of this series exhibit excellent pharmacokinetic properties with long elimination half-lives (7 h) and high oral bioavailability (100%).
Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770
Curtin, Michael L.,Florjancic, Alan S.,Heyman,Michaelides, Michael R.,Garland, Robert B.,Holms, James H.,Steinman, Douglas H.,Dellaria, Joseph F.,Gong, Jane,Wada, Carol K.,Guo, Yan,Elmore, Ildiko B.,Tapang, Paul,Albert, Daniel H.,Magoc, Terrance J.,Marcotte, Patrick A.,Bouska, Jennifer J.,Goodfellow, Carole L.,Bauch, Joy L.,Marsh, Kennan C.,Morgan, Douglas W.,Davidsen, Steven K.
, p. 1557 - 1560 (2007/10/03)
Modification of the biphenyl portion of MMP inhibitor 2a gave analogue 2i which is greater than 1000-fold selective against MMP-2 versus MMP-1. The stereospecific synthesis of both enantiomers of 2i was achieved beginning with (S)- or (R)-benzyl glycidyl ether. The (S)-enantiomer, 11 (ABT-770), is orally bioavailable and efficacious in an in vivo model of tumor growth. Elsevier Science Ltd. All rights reserved.
