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

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.

SUBMITTER: Guduru SKR

PROVIDER: S-EPMC6072512 | biostudies-literature | 2018 Jan

REPOSITORIES: biostudies-literature

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

Guduru Shiva Krishna Reddy SKR Arya Prabhat P

MedChemComm 20171122 1

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 ...[more]

PMID: 30108899

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