Tag Archives: LipE

Discovery of PF-04691502 (PI3K/mTOR dual inhibitor)


Rapamycin and it’s analogues (or rapalogues e.g. CCI-779) modulate the phosphatidylinositol 3-kinase (PI3K) signalling cascade by binding to an allosteric site on the mTORC1 complex (Mammalian target of rapamycin (mTOR), a class IV PI3K protein kinase, forms two functional complexes, … Continue reading

Posted in Clinical Candidates, Enzyme Inhibitors, Kinase Inhibitors, Kinases, Med Chem Strategy | Tagged , , , , , , , , , , , , , , , , , , , , , , , | Leave a comment

Aromatic chloride to nitrile transformation


Introducing a nitrile in the place of less polar substituents is a fairly common approach to reducing lipophilicity in a lead molecule but in this review from the MedChem group at Pfizer the associated benefits of specifically the aromatic chloride to … Continue reading

Posted in Med Chem Strategy, Synthesis | Tagged , , , , , | Leave a comment