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Synthesis and biological evaluation of rapamycin-derived, next generation small molecules
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-11-22 00:00:00 , DOI: 10.1039/c7md00474e
Shiva Krishna Reddy Guduru 1, 2 , Prabhat Arya 3
Affiliation  

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.

中文翻译:

雷帕霉素衍生的下一代小分子的合成和生物学评价

多年来,雷帕霉素因其卓越的生物学特性以及通过与 FKBP-12 结合而成为哺乳动物雷帕霉素靶蛋白 (mTOR) 的有效抑制剂而引起了人们的广泛关注。利用合成和生物合成方法的几种有效策略已被用来开发小分子雷帕霉素类似物或用于合成含有部分雷帕霉素结构的杂合化合物以改善药代动力学特性。在此,我们报告了与雷帕霉素衍生化合物和杂合分子合成相关的精选案例研究,以探索其生物学特性。
更新日期:2017-11-22
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