Articles with "potent" as a keyword



Comparative Effectiveness of Clopidogrel vs. Potent P2Y12 Inhibitors in CYP2C19 Normal Metabolizers Following Percutaneous Coronary Intervention: A Real-World Cohort Study.

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Published in 2025 at "British journal of clinical pharmacology"

DOI: 10.1002/bcp.70373

Abstract: BACKGROUND Evidence suggests that cytochrome P450 2C19 (CYP2C19) genotyping may guide clopidogrel therapy after percutaneous coronary intervention (PCI). However, evidence on the effectiveness of clopidogrel and potent P2Y12 inhibitors (ticagrelor or prasugrel) in patients with… read more here.

Keywords: percutaneous coronary; coronary intervention; effectiveness clopidogrel; potent ... See more keywords

Less necessity of adjuvant S-1 treatment in non-monarchE-eligible patients.

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Published in 2023 at "Cancer medicine"

DOI: 10.1002/cam4.6006

Abstract: BACKGROUND In monarchE and Postoperative Therapy with Endocrine and TS-1 (POTENT) trials, abemaciclib and S-1 have, respectively, shown to be effective as adjuvant therapies for luminal breast cancer (BC), although whether patients who meet the… read more here.

Keywords: eligible patients; potent; monarche eligible; non eligible ... See more keywords

Discovery of a Potent BTK Inhibitor with a Novel Binding Mode by Using Parallel Selections with a DNA‐Encoded Chemical Library

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Published in 2017 at "ChemBioChem"

DOI: 10.1002/cbic.201600573

Abstract: We have identified and characterized novel potent inhibitors of Bruton's tyrosine kinase (BTK) from a single DNA‐encoded library of over 110 million compounds by using multiple parallel selection conditions, including variation in target concentration and… read more here.

Keywords: potent; novel binding; btk; dna encoded ... See more keywords

Design and Synthesis of Potent Ridaifen Analogues: Evaluation as Anticancer, 20S Proteasomal Inhibitors, and Antiebola Virus Agents through In vitro and In Silico Studies

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Published in 2025 at "ChemMedChem"

DOI: 10.1002/cmdc.202500451

Abstract: Ridaifen (RID) analogues are identified as nonpeptide, noncovalent inhibitors of the catalytic subunits of the human 20S proteasome. They demonstrated effectiveness against both multiple myeloma and solid tumors. Herein, the synthesis and biological evaluation of… read more here.

Keywords: ridaifen analogues; ridaifen; potent ridaifen; design synthesis ... See more keywords

Prospective clinical assessment of patients with pulmonary arterial hypertension switched from bosentan to macitentan (POTENT)

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Published in 2022 at "Pulmonary Circulation"

DOI: 10.1002/pul2.12083

Abstract: Abstract Even though pulmonary arterial hypertension (PAH) remains an incurable disease, the combination of PAH‐specific therapies allowed evolving from symptom‐based strategies to others aiming to move patients to low‐risk conditions. Endothelin‐1 (ET‐1) receptor antagonists emerged… read more here.

Keywords: arterial hypertension; macitentan; potent; pulmonary arterial ... See more keywords

Synthesis of 4-alkylaminoimidazo[1,2-a]pyridines linked to carbamate moiety as potent α-glucosidase inhibitors.

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Published in 2020 at "Molecular diversity"

DOI: 10.1007/s11030-020-10137-8

Abstract: In this work, various imidazo[1,2-a]pyridines linked to carbamate moiety were designed, synthesized, and evaluated for their α-glucosidase inhibitory activity. Among synthesized compounds, 4-(3-(tert-Butylamino)imidazo[1,2-a]pyridin-2-yl)phenyl p-tolylcarbamate (6d) was the most potent compound (IC50 = 75.6 µM) compared with acarbose as… read more here.

Keywords: pyridines linked; carbamate moiety; linked carbamate; potent ... See more keywords

A new class of diamide scaffold: Design, synthesis and biological evaluation as potent antimitotic agents, tubulin polymerization inhibition and apoptosis inducing activity studies.

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Published in 2019 at "Bioorganic chemistry"

DOI: 10.1016/j.bioorg.2018.12.007

Abstract: A new series of diamide functional compounds has been designed, synthesized and confirmed by spectroscopic methods and elemental analyses. All the synthesized compounds were evaluated for their antiproliferative activity on HepG2 cell line. Compounds 3k… read more here.

Keywords: new class; apoptosis; class diamide; potent ... See more keywords

Identification of novel 2-(benzo[d]isoxazol-3-yl)-2-oxo-N-phenylacetohydrazonoyl cyanide analoguesas potent EPAC antagonists.

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Published in 2017 at "European journal of medicinal chemistry"

DOI: 10.1016/j.ejmech.2017.04.001

Abstract: Two series of novel EPAC antagonists are designed, synthesized and evaluated in an effort to develop diversified analogues based on the scaffold of the previously identified high-throughput (HTS) hit 1 (ESI-09). Further SAR studies reveal… read more here.

Keywords: novel; epac antagonists; potent epac; identification ... See more keywords

Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFRL858R/T790M inhibitors.

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Published in 2019 at "European journal of medicinal chemistry"

DOI: 10.1016/j.ejmech.2018.11.069

Abstract: Third-generation epidermal growth factor receptor (EGFR)L858R/T790M inhibitors are still the main drugs for the treatment of advanced non-small cell lung cancer (NSCLC), and these drugs have achieved remarkable clinical efficacy. However, there are still many… read more here.

Keywords: design synthesis; t790m inhibitors; t790m; egfrl858r t790m ... See more keywords

Novel thiosemicarbazone derivatives containing indole fragment as potent and selective anticancer agent.

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Published in 2019 at "European journal of medicinal chemistry"

DOI: 10.1016/j.ejmech.2019.111764

Abstract: Potent and safe anticancer drugs research and development are still on the way to human health. In this report, a series of novel thiosemicarbazone derivatives containing indole fragment were designed and synthesized. Most compounds exhibited… read more here.

Keywords: novel thiosemicarbazone; indole fragment; thiosemicarbazone derivatives; derivatives containing ... See more keywords

Structure guided design of potent indole-based ATX inhibitors bearing hydrazone moiety with tumor suppression effects.

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Published in 2020 at "European journal of medicinal chemistry"

DOI: 10.1016/j.ejmech.2020.112456

Abstract: ATX was capable of catalyzing the hydrolysis of LPC to the lipid mediator LPA which attracted considerable attention on the development of potent ATX inhibitors. Herein, driven by the HTS product indole-based lead 1, a… read more here.

Keywords: structure guided; atx inhibitors; moiety; hydrazone moiety ... See more keywords