Literature DB >> 11412980

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

M L Curtin1, 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.   

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.

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Year:  2001        PMID: 11412980     DOI: 10.1016/s0960-894x(01)00032-4

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

Review 1.  Matrix metalloproteinases in the progression of heart failure: potential therapeutic implications.

Authors:  Y Y Li; A M Feldman
Journal:  Drugs       Date:  2001       Impact factor: 9.546

Review 2.  Role of matrix metalloproteinases and therapeutic benefits of their inhibition in spinal cord injury.

Authors:  Haoqian Zhang; Mayland Chang; Christopher N Hansen; D Michele Basso; Linda J Noble-Haeusslein
Journal:  Neurotherapeutics       Date:  2011-04       Impact factor: 7.620

3.  Anti-α-enolase is a prognostic marker in postoperative lung cancer patients.

Authors:  Kuan-Chung Hsiao; Neng-Yao Shih; Pei-Yi Chu; Yi-Mei Hung; Jia-Yi Liao; Shao-Wen Chou; Yi-Yuan Yang; Gee-Chen Chang; Ko-Jiunn Liu
Journal:  Oncotarget       Date:  2015-10-27

4.  Complementary research in mammals and fish indicates MMP-2 as a pleiotropic contributor to optic nerve regeneration.

Authors:  Kim Lemmens; Inge Van Hove; Lieve Moons
Journal:  Neural Regen Res       Date:  2016-05       Impact factor: 5.135

  4 in total

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