Targeting autophagy drug discovery: Targets, indications and development trends.
Jiang M, Wu W, Xiong Z, Yu X, Ye Z, Wu Z.
Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2023.116117 PUBLIKATIONSREGISTRET
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11 träffarDiscovery of pyrazolo[3,4-d]pyrimidines as novel mitogen-activated protein kinase kinase 3 (MKK3) inhibitors.
Takarada JE, Cunha MR, Almeida VM, Vasconcelos SNS, Santiago AS, Godoi PH, Salmazo A, Ramos PZ, Fala AM, de Souza LR, Da Silva IEP, Bengtson MH, Massirer KB, Couñago RM.
Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2023.117561Recent advances in PI3K/PKB/mTOR inhibitors as new anticancer agents.
Occhiuzzi MA, Lico G, Ioele G, De Luca M, Garofalo A, Grande F.
Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2022.114971Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).
Oleksak P, Nepovimova E, Chrienova Z, Musilek K, Patocka J, Kuca K.
Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2022.114498Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.
Raghuvanshi R, Bharate SB.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.0c014674-(Difluoromethyl)-5-(4-((3<i>R</i>,5<i>S</i>)-3,5-dimethylmorpholino)-6-((<i>R</i>)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders.
Borsari C, Keles E, Rageot D, Treyer A, Bohnacker T, Bissegger L, De Pascale M, Melone A, Sriramaratnam R, Beaufils F, Hamburger M, Hebeisen P, Löscher W, Fabbro D, Hillmann P, Wymann MP.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.0c00620Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.
Rageot D, Bohnacker T, Melone A, Langlois JB, Borsari C, Hillmann P, Sele AM, Beaufils F, Zvelebil M, Hebeisen P, Löscher W, Burke J, Fabbro D, Wymann MP.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.8b01262The target landscape of clinical kinase drugs.
Klaeger S, Heinzlmeir S, Wilhelm M, Polzer H, Vick B, Koenig PA, Reinecke M, Ruprecht B, Petzoldt S, Meng C, Zecha J, Reiter K, Qiao H, Helm D, Koch H, Schoof M, Canevari G, Casale E, Depaolini SR, Feuchtinger A, Wu Z, Schmidt T, Rueckert L, Becker W, Huenges J, Garz AK, Gohlke BO, Zolg DP, Kayser G, Vooder T, Preissner R, Hahne H, Tõnisson N, Kramer K, Götze K, Bassermann F, Schlegl J, Ehrlich HC, Aiche S, Walch A, Greif PA, Schneider S, Felder ER, Ruland J, Médard G, Jeremias I, Spiekermann K, Kuster B.
Science · research support, non-u.s. gov't; research-article; journal article · DOI 10.1126/science.aan4368Design, synthesis and SAR of new-di-substituted pyridopyrimidines as ATP-competitive dual PI3Kα/mTOR inhibitors.
Al-Ashmawy AAK, Ragab FA, Elokely KM, Anwar MM, Perez-Leal O, Rico MC, Gordon J, Bichenkov E, Mateo G, Kassem EMM, Hegazy GH, Abou-Gharbia M, Childers W.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2017.05.044Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2.
Pike KG, Morris J, Ruston L, Pass SL, Greenwood R, Williams EJ, Demeritt J, Culshaw JD, Gill K, Pass M, Finlay MR, Good CJ, Roberts CA, Currie GS, Blades K, Eden JM, Pearson SE.
J Med Chem · journal article · DOI 10.1021/jm501778sOptimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.
Pike KG, Malagu K, Hummersone MG, Menear KA, Duggan HM, Gomez S, Martin NM, Ruston L, Pass SL, Pass M.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2013.01.019