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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Curtin ML,Florjancic AS,Heyman HR,Michaelides MR,Garland RB,Holms JH,Steinman DH,Dellaria JF,Gong J,Wada CK,Guo Y,Elmore IB,Tapang P,Albert DH,Magoc TJ,Marcotte PA,Bouska JJ,Goodfellow CL,Bauch JL,Marsh KC,Morgan

doi

10.1016/s0960-894x(01)00032-4

subject

Has Abstract

pub_date

2001-06-18 00:00:00

pages

1557-60

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960894X01000324

journal_volume

11

pub_type

杂志文章

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