The phosphoinositide 3-kinases (PI3Ks) are lipid kinases that play a central role in control of cell growth,
proliferation, migration, survival and angiogenesis, and drive the progression of tumors by activating phosphoinositidedependent
kinase, protein kinase B (Akt) and the mammalian target of rapamycin (mTOR). The PI3K/Akt/mTOR
pathway has been shown to play an important role in cancer and has become an important target for anticancer drug
development. An interest in targeting two important points along this critical signaling pathway has spurred the
development of dual PI3K/mTOR inhibitors that could both prevent cancer cell proliferation and induce programmed cell
death (apoptosis) by fully suppressing Akt activation. This review summarizes the developments of a diversity of small
molecule dual PI3K/mTOR inhibitors in recent 10 years, with an emphasis on their structural features, the relevant
biological activities, and the structure-activity relationships (SARs).
Keywords: Anticancer, anticancer agents, cancer, dual PI3K/mTOR kinase inhibitors, kinase inhibitors, PI3K, PI3K,
PI3K/Akt/mTOR, PI3K signaling pathway, mTOR, structure-activity relationships, SARs.
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