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Identification of 3-amidoquinoline derivatives as PI3K/mTOR dual inhibitors with potential for cancer therapy
A new series of 3-amidoquinoline derivatives were designed, synthesized and evaluated as PI3K/mTOR dual inhibitors. Among them, five compounds showed potent PI3Kalpha inhibitory activities (IC50 < 10 nM) and anti-proliferative activities (IC50 < 1 muM). The representative compound 15a can significantly inhibit other class I PI3Ks, mTOR and phosphorylation of pAkt(Ser473) at low nanomolar level, suggesting that 15a was a potent PI3K/mTOR dual inhibitor. Moreover, 15a displayed favorable pharmacokinetic properties in vivo. Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Computed Properties of C3H2BrNO, you can also check out more blogs about97925-43-4
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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem