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Bioorg Med Chem Lett. 2001 Jun 18;11(12):1557-60.

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

Author information

1
Cancer Research Area, Abbott Laboratories, Dept. 47J, Bldg. AP10, 100 Abbott Park Road, Abbott Park, IL 60064, USA. mike.curtin@abbott.com

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.

PMID:
11412980
[Indexed for MEDLINE]

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