Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines.

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Published in Biochemistry on June 19, 2001

Authors

G Tian1, M Cory, A A Smith, W B Knight

Author Affiliations

1: Department of Molecular Biochemistry, GlaxoSmithKline Research and Development, Research Triangle Park, North Carolina 27709, USA. gaochao.tian@astrazeneca.com

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Irreversible enzyme inhibitors. CLXV. Proteolytic enzymes. XV. Inhibition of guinea pig complement by derivatives of m-phenoxypropoxybenzamidine. J Med Chem (1969) 0.79

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Orally active beta-lactam inhibitors of human leukocyte elastase. 2. Effect of C-4 substitution. J Med Chem (1993) 0.78

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