Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 22, 1998, Pages 3203-3206

  Carroll, Carolyn DiIanni ^a   Johnson, Theodore O ^a   Tao, Shewei ^a   Lauri, Giorgio ^a   Orlowski, Marc ^a   Gluzman, Ilya Y ^b   Goldberg, Daniel E ^b   Dolle, Roland E ^a  

^a PHARMACOPEIA INC   (United States)

^b WASHINGTON UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMIDE; CATHEPSIN D; PLASMEPSIN II; PROTEINASE; STATINE; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; CRYSTAL STRUCTURE; ENZYME ACTIVE SITE; ENZYME ASSAY; FREQUENCY ANALYSIS; LIBRARY; PURIFICATION; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

EID: 0032542040     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00554-X     Document Type: Article

References (10)

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3. 3. Carroll, C. D.; Patel, H.; Johnson, T. O.; Guo, T.; Orlowski, M.; He, Z.-M.; Cavallaro, C. L.; Guo, J.; Oksman, A.; Gluzman, I. Y.; Connelly, J.; Chelsky, D.; Goldberg, D. E.; Dolle, R. E. Bioorg. & Med. Chem. Lett. 1998, 8, 2315.
4. 4. Computational docking studies were performed using MacroModel BatchMin 5.0 and the cathepsin D X-ray structure, 1LYB ref 5.
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10. 50 value of 3 μM against Plasmodium falciparum in cell culture. (Desjardin, R. E.; Canfield, R. J.; Haynes, J. D.; Chulay, J. D.; Antimicrob. Agents Chemother. 1979, 16, 710.)