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NaClO‐Mediated Cross Installation of Indoles and Azoles Benefits Anticancer Hit Discovery

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A rapid, effective NaClO-mediated cross installation of indoles and azoles for the construction of various N-linked 2-(azol-1-yl) indole derivatives and the late-stage functional modification of drugs and peptides has been developed, which can benefit anticancer hit discovery.


Abstract

Innovations in synthetic chemistry have a profound impact on the drug discovery process, and will always be a necessary driver of drug development. As a result, it is of significance to develop novel simple and effective synthetic installation of medicinal modules to promote drug discovery. Herein, we have developed a NaClO-mediated cross installation of indoles and azoles, both of which are frequently encountered in drugs and natural products. This effective toolbox provides a convenient synthetic route to access a library of N-linked 2-(azol-1-yl) indole derivatives, and can be used for late-stage modification of drugs, natural products and peptides. Moreover, biological screening of the library has revealed that several adducts showed promising anticancer activities against A549 and NCI-H1975 cells, which give us a hit for anticancer drug discovery.

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