Less necessity of adjuvant S-1 treatment in non-monarchE-eligible patients.
Sign Up to like & getrecommendations! 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
Sign Up to like & getrecommendations! 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
Prospective clinical assessment of patients with pulmonary arterial hypertension switched from bosentan to macitentan (POTENT)
Sign Up to like & getrecommendations! 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.
Sign Up to like & getrecommendations! 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.
Sign Up to like & getrecommendations! 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.
Sign Up to like & getrecommendations! 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.
Sign Up to like & getrecommendations! 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.
Sign Up to like & getrecommendations! 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.
Sign Up to like & getrecommendations! 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
Discovery of a potent, highly selective, and orally bioavailable inhibitor of CDK8 through a structure-based optimisation.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113391
Abstract: CDK8 is deregulated in multiple types of human cancer and is viewed as a therapeutic target for the treatment of the disease. Accordingly, the search for small-molecule inhibitors of CDK8 is being intensified. Capitalising on… read more here.
Keywords: inhibitor; based optimisation; cdk8; structure based ... See more keywords
Development of Potent Nanosized Isatin-isonicotinohydrazide Hybrid for Management of Mycobacterium Tuberculosis.
Sign Up to like & getrecommendations! Published in 2021 at "International journal of pharmaceutics"
DOI: 10.1016/j.ijpharm.2021.121369
Abstract: Inspired by the antitubercular activity of isoniazid (INH) and 5-bromoisatin, isatin-INH hybrid (WF-208) has been synthesized as a potent agent against multidrug-resistant (MDR) and extensively drug-resistant (XDR) strains of M. tuberculosis. In silico molecular docking… read more here.
Keywords: development potent; potent nanosized; tuberculosis; compound ... See more keywords