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Volumn 120, Issue 29, 1998, Pages 7220-7225

Multistep convergent solution-phase combinatorial synthesis and deletion synthesis deconvolution

Author keywords

[No Author keywords available]

Indexed keywords

ALKENE; AMIDE; DIGLYCINE DERIVATIVE TC 99M;

EID: 3543025082     PISSN: 00027863     EISSN: None     Source Type: Journal    
DOI: 10.1021/ja9803557     Document Type: Article
Times cited : (68)

References (69)
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    • The combination of two nonidentical libraries of x and y members provides x × y members. When a library of x members is symmetrically dimerized, the combination provides x(x+1)/2 members. With A1-A10, B1-B10, C1-C4: for 9, n = (100 × 101/2) × 4. For 10, n = (100 × 101/2) × 20 + {(100 × 101/2)[(100 × 101/2) - 1]/2} × 32. For 11, n = (100 × 101/2) × 9 + {(100 × 101/2)[(100 × 101/2) - 1]/2} × 9.
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    • This is true in the generalized case when a single residue within the library is incorporated once at a unique location. With dimerization libraries such as those disclosed herein, scanning deconvolution would fail to detect unique activities for unsymmetrical incorporations, e.g., structures containing both A1 and A5. Here, deletion deconvolution sublibraries are required and would be expected to detect a loss of activity with the sublibraries lacking A1 and A5. In the example provided in Table 3 for 9, the number of compounds insensitive to scanning deconvolution is 800 out of 1300, while in principle all are sensitive to deletion deconvolution. Expanding this to the 20 200 compounds in 9 prepared from A1-A10, B1-B10, and C1-C4, 16 200 out of 20 200 compounds are insensitive to scanning deconvolution.


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