Search Results - "Torrice, Chad D"
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SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK)
Published in Journal of medicinal chemistry (14-03-2019)“…We describe SGC-GAK-1 (11), a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK), together with a structurally related negative…”
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Optimization of the 4-anilinoquin(az)oline scaffold as epidermal growth factor receptor (EGFR) inhibitors for chordoma utilizing a toxicology profiling assay platform
Published in Scientific reports (27-07-2022)“…The 4-anilinoquin(az)oline is a well-known kinase inhibitor scaffold incorporated in clinical inhibitors including gefitinib, erlotinib, afatinib, and…”
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3
Mitigation of hematologic radiation toxicity in mice through pharmacological quiescence induced by CDK4/6 inhibition
Published in The Journal of clinical investigation (01-07-2010)“…Total body irradiation (TBI) can induce lethal myelosuppression, due to the sensitivity of proliferating hematopoietic stem/progenitor cells (HSPCs) to…”
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Synthesis and Evaluation of Novel 1,2,6-Thiadiazinone Kinase Inhibitors as Potent Inhibitors of Solid Tumors
Published in Molecules (Basel, Switzerland) (29-09-2021)“…A focused series of substituted 4H-1,2,6-thiadiazin-4-ones was designed and synthesized to probe the anti-cancer properties of this scaffold. Insights from…”
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Influence of Germline Genetics on Tacrolimus Pharmacokinetics and Pharmacodynamics in Allogeneic Hematopoietic Stem Cell Transplant Patients
Published in International journal of molecular sciences (29-01-2020)“…Tacrolimus exhibits high inter-patient pharmacokinetics (PK) variability, as well as a narrow therapeutic index, and therefore requires therapeutic drug…”
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Evaluation of the performance of a prior tacrolimus population pharmacokinetic kidney transplant model among adult allogeneic hematopoietic stem cell transplant patients
Published in Clinical and translational science (01-05-2021)“…Tacrolimus is a calcineurin inhibitor used to prevent acute graft versus host disease in adult patients receiving allogeneic hematopoietic stem cell…”
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Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines
Published in Bioorganic & medicinal chemistry letters (15-09-2019)“…We screened a series of 4-anilinoquinolines and 4-anilinoquinazolines and identified novel inhibitors of Mycobacterium tuberculosis (Mtb). The focused…”
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Pharmacokinetics and Pharmacodynamics of Apixaban in Nephrotic Syndrome: Findings From a Phase 1a Trial
Published in American journal of kidney diseases (01-03-2023)Get full text
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Design and evaluation of 1,2,3-dithiazoles and fused 1,2,4-dithiazines as anti-cancer agents
Published in Bioorganic & medicinal chemistry letters (01-07-2021)“…[Display omitted] Heteroatom rich 1,2,3-dithiazoles are relatively underexplored in medicinal chemistry. We now report screening data on a series of…”
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Targeting an EGFR Water Network with 4‐Anilinoquin(az)oline Inhibitors for Chordoma
Published in ChemMedChem (04-10-2019)“…Quinoline‐ and quinazoline‐based kinase inhibitors of the epidermal growth factor receptor (EGFR) have been used to target non‐small cell lung cancer (NSCLC)…”
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A New Chemotype of Chemically Tractable Nonsteroidal Estrogens Based on a Thieno[2,3‑d]pyrimidine Core
Published in ACS medicinal chemistry letters (14-07-2022)“…Despite continued interest in the development of nonsteroidal estrogens and antiestrogens, there are only a few chemotypes of estrogen receptor ligands. Using…”
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Abstract 1743: Evaluation of the effects of combined chemical inhibition of PARP and BET proteins in preclinical models of urothelial bladder cancer
Published in Cancer research (Chicago, Ill.) (15-08-2020)“…Abstract Purpose: Metastatic urothelial bladder cancer (mUC) is incurable, and options are limited after patients fail 1st and 2nd line treatments. Thus, there…”
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Structural Determinants of the Binding and Activation of Estrogen Receptor α by Phenolic Thienopyrimidines
Published in Helvetica chimica acta (01-09-2023)“…Synthetic, structural, and computational approaches were used to solve the puzzle as to how a phenolic nonsteroidal estrogen 1 with only a single H‐bond to its…”
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Structural Determinants of the Binding and Activation of Estrogen Receptor α by Phenolic Thieno[2,3‐ d ]pyrimidines
Published in Helvetica chimica acta (01-09-2023)“…Abstract Synthetic, structural, and computational approaches were used to solve the puzzle as to how a phenolic nonsteroidal estrogen 1 with only a single…”
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Application of a Tacrolimus Population Pharmacokinetic Model to Adult Allogeneic Hematopoietic Stem Cell Transplant Patients
Published in Transplantation and cellular therapy (01-03-2021)Get full text
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