Facile Synthesis of Rapamycin-Peptide Conjugates as mTOR and Akt inhibitor.

The simple and straightforward process for the synthesis of rapamycin peptide conjugate in regio and chemoselective manner was developed. The methodology comprises tagging of chemoselective functionalities to rapamycin and peptides which enables conjugation of free peptides without protecting side chain amino acids functionality in high yield and purity. From this methodology we were successfully conjugate free peptides containing upto 15 amino acids. Rapamycin is also conjugated to the peptides known for inhibiting the kinase activity of Akt protein. These conjugates act as dual target inhibitor and inhibit the kinase activity of both mTOR and Akt