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

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

  • Bioorg Med Chem Lett. 2001 Jun 18;11(12):1557-60. doi: 10.1016/s0960-894x(01)00032-4.
M L Curtin 1,  A S Florjancic,  H R Heyman,  M R Michaelides,  R B Garland,  J H Holms,  D H Steinman,  J F Dellaria,  J Gong,  C K Wada,  Y Guo,  I B Elmore,  P Tapang,  D H Albert,  T J Magoc,  P A Marcotte,  J J Bouska,  C L Goodfellow,  J L Bauch,  K C Marsh,  D W Morgan,  S K Davidsen
Affiliations

Affiliation

  • 1 Cancer Research Area, Abbott Laboratories, Dept. 47J, Bldg. AP10, 100 Abbott Park Road, Abbott Park, IL 60064, USA. mike.curtin@abbott.com
PMID: 11412980 DOI: 10.1016/s0960-894x(01)00032-4
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-123130
    MMP2 Inhibitor
    MMP