期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 11, 期 12, 页码 1557-1560出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(01)00032-4
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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. (C) 2001 Elsevier Science Ltd. All rights reserved.
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