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A natural product based DOS library of hybrid systemsPublished in Elsevier Masson SAS
2015
PMID: 25794788
Volume: 95
Pages: 41 - 48
Here we described a natural product inspired modular DOS strategy for the synthesis of a library of hybrid systems that are structurally and stereochemically disparate. The main scaffold is a pyrroloisoquinoline motif, that is synthesized from tandem Pictet-Spengler lactamization. The structural diversity is generated via privileged scaffolds that are attached at the appropriate site of the motif. Screening of the library compounds for their antiplasmodial activity against chloroquine sensitive 3D7 cells indicated few compounds with moderate activity (20-50 μM). A systematic comparison of structural intricacy between the library members and a natural product dataset obtained from ZINC® revealed comparable complexity. © 2015 Elsevier Masson SAS.
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Published in Elsevier Masson SAS
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