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Synthesis and biological evaluation of rapamycin-derived, next generation small molecules

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Abstract

Over the years, rapamycin has attracted serious attention due to its remarkable biological properties and as a potent inhibitor of the mammalian target of rapamycin (mTOR) protein through its binding with FKBP-12. Several efficient strategies that utilize synthetic and biosynthetic approaches have been utilized to develop small molecule rapamycin analogs or for synthesizing hybrid compounds containing a partial rapamycin structure to improve pharmacokinetic properties. Herein, we report selected case studies related to the synthesis of rapamycin-derived compounds and hybrid molecules to explore their biological properties.

Graphical abstract: Synthesis and biological evaluation of rapamycin-derived, next generation small molecules

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Publication details

The article was received on 17 Sep 2017, accepted on 21 Nov 2017 and first published on 22 Nov 2017


Article type: Review Article
DOI: 10.1039/C7MD00474E
Citation: Med. Chem. Commun., 2018, Advance Article
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    Synthesis and biological evaluation of rapamycin-derived, next generation small molecules

    S. K. R. Guduru and P. Arya, Med. Chem. Commun., 2018, Advance Article , DOI: 10.1039/C7MD00474E

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