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Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids.

ABSTRACT: The archazolids are potent antiproliferative compounds that have recently emerged as a novel class of promising anticancer agents. Their complex macrolide structures and scarce natural supply make the development of more readily available analogues highly important. Herein, we report the design, synthesis and biological evaluation of four simplified and partially saturated archazolid derivatives. We also reveal important structure-activity relationship data as well as insights into the pharmacophore of these complex polyketides.

SUBMITTER: Riviere S

PROVIDER: S-EPMC7496434 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature

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Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids.

Rivière Solenne S Vielmuth Christin C Ennenbach Christiane C Abdelrahman Aliaa A Lemke Carina C Gütschow Michael M Müller Christa E CE Menche Dirk D

ChemMedChem 20200610 14

The archazolids are potent antiproliferative compounds that have recently emerged as a novel class of promising anticancer agents. Their complex macrolide structures and scarce natural supply make the development of more readily available analogues highly important. Herein, we report the design, synthesis and biological evaluation of four simplified and partially saturated archazolid derivatives. We also reveal important structure-activity relationship data as well as insights into the pharmacop ...[more]

PMID: 32363789

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