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Potent, Selective, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin Kinase Domain Exhibiting Single Agent Antiproliferative Activity

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What this work says

Outgoing claims: the papers this work cites, builds on, or argues with.

inferredcites →https://doi.org/10.1016/j.bmcl.2009.08.038openalex-snapshot

The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase

inferredcites →https://doi.org/10.1016/j.bmcl.2009.08.069openalex-snapshot

Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR

inferredcites →https://doi.org/10.1016/j.bmcl.2009.10.075openalex-snapshot

Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K

inferredcites →https://doi.org/10.1016/j.bmcl.2009.11.050openalex-snapshot

Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)

inferredcites →https://doi.org/10.1016/j.bmcl.2009.12.086openalex-snapshot

Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 1-substituent

inferredcites →https://doi.org/10.1016/j.bmcl.2010.02.012openalex-snapshot

4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)

inferredcites →https://doi.org/10.1016/j.bmcl.2010.02.029openalex-snapshot

Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kα

inferredcites →https://doi.org/10.1016/j.bmcl.2010.02.045openalex-snapshot

Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors

inferredcites →https://doi.org/10.1016/j.bmcl.2011.01.139openalex-snapshot

Imidazo[1,5-a]pyrazines: Orally efficacious inhibitors of mTORC1 and mTORC2

inferredcites →https://doi.org/10.1016/j.bmcl.2011.02.007openalex-snapshot

Discovery of triazine-benzimidazoles as selective inhibitors of mTOR

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Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability

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Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitors

inferredcites →https://doi.org/10.1016/j.bmcl.2012.04.036openalex-snapshot

Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor

inferredcites →https://doi.org/10.1016/j.bmcl.2012.05.104openalex-snapshot

Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors

inferredcites →https://doi.org/10.1016/j.bmcl.2012.06.033openalex-snapshot

Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors

inferredcites →https://doi.org/10.1021/jm0605233openalex-snapshot

Matched Molecular Pairs as a Guide in the Optimization of Pharmaceutical Properties; a Study of Aqueous Solubility, Plasma Protein Binding and Oral Exposure

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Discovery of 1-(4-(4-Propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a Highly Potent, Selective Mammalian Target of Rapamycin (mTOR) Inhibitor for the Treatment of Cancer

inferredcites →https://doi.org/10.1021/jm101520vopenalex-snapshot

Discovery of 9-(6-Aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a Potent, Selective, and Orally Available Mammalian Target of Rapamycin (mTOR) Inhibitor for Treatment of Cancer

inferredcites →https://doi.org/10.1021/jm200215yopenalex-snapshot

Potent, Selective, and Orally Bioavailable Inhibitors of Mammalian Target of Rapamycin (mTOR) Kinase Based on a Quaternary Substituted Dihydrofuropyrimidine

inferredcites →https://doi.org/10.1021/jm2009327openalex-snapshot

Discovery of a Potent, Selective, and Orally Available Class I Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor (GDC-0980) for the Treatment of Cancer

inferredcites →https://doi.org/10.1021/jm800295dopenalex-snapshot

The Identification of 2-(1 H -Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2- d ]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer

inferredcites →https://doi.org/10.1021/jm900851fopenalex-snapshot

ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective Pyrazolopyrimidines

inferredcites →https://doi.org/10.1021/jm9012642openalex-snapshot

Discovery of Potent and Selective Inhibitors of the Mammalian Target of Rapamycin (mTOR) Kinase

inferredcites →https://doi.org/10.1021/jm901284wopenalex-snapshot

Discovery of (Thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer

inferredcites →https://doi.org/10.1021/jm901415xopenalex-snapshot

Morpholine Derivatives Greatly Enhance the Selectivity of Mammalian Target of Rapamycin (mTOR) Inhibitors

inferredcites →https://doi.org/10.1038/nrc1974openalex-snapshot

mTOR and cancer: insights into a complex relationship

inferredcites →https://doi.org/10.1042/bj20090489openalex-snapshot

Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR)

inferredcites →https://doi.org/10.1055/s-1993-22398openalex-snapshot

Mild and Selective Debenzylation of Tertiary Amines Using α-Chloroethyl Chloroformate

inferredcites →https://doi.org/10.1056/nejmoa1109653openalex-snapshot

Everolimus in Postmenopausal Hormone-Receptor–Positive Advanced Breast Cancer

inferredcites →https://doi.org/10.1158/0008-5472.can-09-0299openalex-snapshot

Biochemical, Cellular, and In vivo Activity of Novel ATP-Competitive and Selective Inhibitors of the Mammalian Target of Rapamycin

inferredcites →https://doi.org/10.1158/0008-5472.can-09-1751openalex-snapshot

AZD8055 Is a Potent, Selective, and Orally Bioavailable ATP-Competitive Mammalian Target of Rapamycin Kinase Inhibitor with In vitro and In vivo Antitumor Activity

inferredcites →https://doi.org/10.1158/1078-0432.ccr-06-0118openalex-snapshot

A Phase I and Pharmacokinetic Study of Temsirolimus (CCI-779) Administered Intravenously Daily for 5 Days Every 2 Weeks to Patients with Advanced Cancer

inferredcites →https://doi.org/10.1158/1535-7163.mct-10-1099openalex-snapshot

Preclinical Characterization of OSI-027, a Potent and Selective Inhibitor of mTORC1 and mTORC2: Distinct from Rapamycin

inferredcites →https://doi.org/10.1158/1535-7163.mct-11-0446openalex-snapshot

GDC-0980 Is a Novel Class I PI3K/mTOR Kinase Inhibitor with Robust Activity in Cancer Models Driven by the PI3K Pathway

inferredcites →https://doi.org/10.1200/jco.2007.14.5482openalex-snapshot

Dose- and Schedule-Dependent Inhibition of the Mammalian Target of Rapamycin Pathway With Everolimus: A Phase I Tumor Pharmacodynamic Study in Patients With Advanced Solid Tumors

inferredcites →https://doi.org/10.1371/journal.pbio.1000038openalex-snapshot

Active-Site Inhibitors of mTOR Target Rapamycin-Resistant Outputs of mTORC1 and mTORC2

inferredcites →https://doi.org/10.1371/journal.pmed.0050008openalex-snapshot

Antitumor Activity of Rapamycin in a Phase I Trial for Patients with Recurrent PTEN-Deficient Glioblastoma

inferredcites →https://doi.org/10.2174/187231211796905017openalex-snapshot

High-Throughput, 384-Well, LC-MS/MS CYP Inhibition Assay Using Automation, Cassette-Analysis Technique and Streamlined Data Analysis

What points at this work

Incoming claims: where this work appears in other papers’ reference lists and arguments.

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Design, Synthesis, Characterization, Molecular Docking Studies and Biological Evaluation of 5, 6, 7, 8-Tetrahydropyrido[3,4-D]Pyrimidine Derivatives as Antimicrobial Agents

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Design, Synthesis, Biological Evaluation and Molecular Docking Studies of Tetrahydropyrido[3, 4-D]Pyrimidine Derivatives as Anti-Leukemic Agents

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Mechanistic/mammalian target of rapamycin: Recent pathological aspects and inhibitors

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3D-QSAR, molecular dynamics simulations, and molecular docking studies on pyridoaminotropanes and tetrahydroquinazoline as mTOR inhibitors

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Design, synthesis, anticancer activity and docking studies of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as mTOR inhibitors

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Discovery of a novel class anti-proliferative agents and potential inhibitors of EGFR tyrosine kinases based on 4-anilinotetrahydropyrido[4,3-d]pyrimidine scaffold: Design, synthesis and biological evaluations

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Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation

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A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors

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Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy

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Design, synthesis, and biological evaluation of imidazo[1,2- b ]pyridazine derivatives as mTOR inhibitors

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Synthesis and biological evaluation of 2,6-disubstituted-9H-purine, 2,4-disubstitued-thieno[3,2-d]pyrimidine and -7H-pyrrolo[2,3-d]pyrimidine analogues as novel CHK1 inhibitors

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Design and synthesis of (2-(phenylamino)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone analogues as potent anti-tubulin polymerization agents

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Targeting mTOR for fighting diseases: A revisited review of mTOR inhibitors

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A new strategy for hit generation: Novel in cellulo active inhibitors of CYP121A1 from Mycobacterium tuberculosis via a combined X-ray crystallographic and phenotypic screening approach (XP screen)

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Design, synthesis and antitumor evaluation of novel quinazoline analogs in hepatocellular carcinoma cell

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Synthesis, biological evaluation and molecular docking studies of tetrahydropyrido[3, 4-d]pyrimidine derivatives as anti-leukemic agents

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Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)

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Pyrimidoaminotropanes as Potent, Selective, and Efficacious Small Molecule Kinase Inhibitors of the Mammalian Target of Rapamycin (mTOR)

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Phosphatidylinositol 3-Kinase (PI3K) and Phosphatidylinositol 3-Kinase-Related Kinase (PIKK) Inhibitors: Importance of the Morpholine Ring

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Discovery of (2S)-8-[(3R)-3-Methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido[1,2-a]pyrimidin-6-one: A Novel Potent and Selective Inhibitor of Vps34 for the Treatment of Solid Tumors

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Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349

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Furthering the design and the discovery of small molecule ATP-competitive mTOR inhibitors as an effective cancer treatment

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Multimodal Microvascular Imaging Reveals that Selective Inhibition of Class I PI3K Is Sufficient to Induce an Antivascular Response

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Recent development of ATP-competitive small molecule phosphatidylinostitol-3-kinase inhibitors as anticancer agents

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Synthesis of 5-(4-Morpholino-7, 8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-2-yl)pyridin-2-amine

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Overview of Research into mTOR Inhibitors

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