Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.

Abstract

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.

Cite this paper

@article{Curtin2001DiscoveryAC, title={Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.}, author={Michael Curtin and Alan S Florjancic and H Robin Heyman and Michael Michaelides and Robert B Garland and James H Holms and Douglas H Steinman and Joseph F Dellaria and Jian Ping Gong and Carol K Wada and Y Guo and I B Elmore and Paul H Tapang and Daniel H. Albert and Terrance J Magoc and Patrick A Marcotte and Jennifer J. Bouska and Carole L Goodfellow and Joy L. Bauch and Kennan C. Marsh and Douglas W. Morgan and Steven K. Davidsen}, journal={Bioorganic & medicinal chemistry letters}, year={2001}, volume={11 12}, pages={1557-60} }