Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale

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SUMMARY

    The authors synthesized scaffolds that contained three amino_acids: one with a primary amine in the side chain (chosen from six amino_acids); one α-amino_acid with a random side chain (chosen from 15 amino_acids); and one with a random backbone structure (chosen from six amino_acids) (Fig 2b and c; scaffold formats 1a-f). Of the 3,780 scaffolds that could theoretically be assembled based on the indicated formats and amino_acid building blocks, the authors synthesized 384 randomly chosen ones, or 10%. The best three hits, M1, M2, and M3, were all structurally similar and based on . . .

     

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