A natural product based DOS library of hybrid systems

European Journal of Medicinal Chemistry
Ganesh PrabhuSubhabrata Sen

Abstract

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.

References

Aug 20, 1976·Science·W Trager, J B Jensen
Aug 24, 2004·Combinatorial Chemistry & High Throughput Screening·R W DeSimoneD A Pippin
Sep 4, 2010·Science·Matthias RottmannThierry T Diagana

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Citations

Feb 3, 2016·Chemical & Pharmaceutical Bulletin·Sol Romina MartínezMaría Cecilia Becerra
Dec 6, 2018·Organic & Biomolecular Chemistry·Shuang-Jiang MaQiang Zhang
Jan 23, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Andrea CalcaterraFrancesca Ghirga

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