LAUSR

Ebselen oxide and derivatives are new allosteric HER2 inhibitors for HER2-positive cancers.

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2 Published in 2023 at "Molecular oncology"

DOI: 10.1002/1878-0261.13419

Abstract: Human epidermal growth factor receptor 2 (ErbB2/HER2) is a tyrosine kinase receptor that is overexpressed in 25% of primary human breast cancers, as well as in multiple other cancers. HER2-targeted therapies improved progression-free and overall… read more here.

Keywords: ebselen oxide; oxide derivatives; her2; new allosteric ... See more keywords

Synthesis and Docking of Novel 3‐Indolylpropyl Derivatives as New Polypharmacological Agents Displaying Affinity for 5‐HT1AR/SERT

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1 Published in 2017 at "Archiv der Pharmazie"

DOI: 10.1002/ardp.201600271

Abstract: A series of novel 3‐indolylpropyl derivatives was synthesized and evaluated for their binding affinities at the serotonin‐1A receptor subtype (5‐HT1AR) and the 5‐HT transporter (SERT). Compounds 11b and 14b exhibited the highest affinities at the… read more here.

Keywords: ht1ar; synthesis docking; indolylpropyl derivatives; novel indolylpropyl ... See more keywords

N‐Substituted pyrimidinethione and acetophenone derivatives as a new therapeutic approach in diabetes

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0 Published in 2020 at "Archiv der Pharmazie"

DOI: 10.1002/ardp.202000075

Abstract: In this study, compounds with 4‐hydroxybutyl, 4‐phenyl, 5‐carboxylate, and pyrimidine moieties were determined as α‐glycosidase inhibitors. N‐Substituted pyrimidinethione and acetophenone derivatives (A1–A5, B1–B11, and C1–C11) were good inhibitors of the α‐glycosidase enzyme, with Ki values… read more here.

Keywords: substituted pyrimidinethione; pyrimidinethione; acetophenone derivatives; derivatives new ... See more keywords

C2‐Modified Sparteine Derivatives Are a New Class of Potentially Long‐Acting Sodium Channel Blockers

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1 Published in 2017 at "ChemMedChem"

DOI: 10.1002/cmdc.201700568

Abstract: The lupin alkaloid sparteine is a well‐known chiral diamine with a range of applications in asymmetric synthesis, as well as a blocker of voltage‐gated sodium channels (VGSCs). However, there is only scarce information on the… read more here.

Keywords: new class; modified sparteine; sparteine derivatives; sodium ... See more keywords

Multitarget Hybrid Fasudil Derivatives as a New Approach to the Potential Treatment of Amyotrophic Lateral Sclerosis

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1 Published in 2022 at "Journal of Medicinal Chemistry"

DOI: 10.1021/acs.jmedchem.1c01255

Abstract: Hybrid compounds containing structural fragments of the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids were designed with the aid of docking and molecular mechanics studies. Following the synthesis of the… read more here.

Keywords: fasudil; hybrid fasudil; multitarget; multitarget hybrid ... See more keywords

Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors.

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1 Published in 2022 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.2c01346

Abstract: The receptor tyrosine kinase AXL is a promising target for anticancer drug discovery. Herein, we describe the discovery of 3-aminopyrazole derivatives as new potent and selective AXL kinase inhibitors. One of the representative compounds, 6li,… read more here.

Keywords: new potent; aminopyrazole derivatives; axl; discovery aminopyrazole ... See more keywords

2-Aminopyrimidine Derivatives as New Selective Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors.

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1 Published in 2017 at "ACS medicinal chemistry letters"

DOI: 10.1021/acsmedchemlett.7b00091

Abstract: A series of 2-aminopyrimidine derivatives were designed and synthesized as highly selective FGFR4 inhibitors. One of the most promising compounds 2n tightly bound FGFR4 with a Kd value of 3.3 nM and potently inhibited its… read more here.

Keywords: new selective; aminopyrimidine derivatives; fgfr4 inhibitors; derivatives new ... See more keywords

Hydroxylamine Derivatives as a New Paradigm in the Search of Antibacterial Agents

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0 Published in 2018 at "ACS Omega"

DOI: 10.1021/acsomega.8b01384

Abstract: Serious infections caused by bacteria that are resistant to commonly used antibiotics have become a major global healthcare problem in the 21st century. Multidrug-resistant bacteria causing severe infections mainly grow in complex bacterial communities known… read more here.

Keywords: antibacterial agents; search antibacterial; hydroxylamine derivatives; paradigm search ... See more keywords

7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity.

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0 Published in 2018 at "MedChemComm"

DOI: 10.1039/c8md00352a

Abstract: A series of new semi-synthetic 7-deacetyl-10-alkylthiocolchicne derivatives with ethyl, n-propyl, i-propyl and n-butyl substituents were synthesised and characterised by spectroscopic methods, elemental analysis, DFT calculations and molecular docking simulations. All the synthesized compounds have been… read more here.

Keywords: alkylthiocolchicine derivatives; deacetyl alkylthiocolchicine; fungicidal activity; derivatives new ... See more keywords

3(2H)-pyridazinone derivatives: a new scaffold for novel plant activators

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1 Published in 2019 at "RSC Advances"

DOI: 10.1039/c9ra06892a

Abstract: Due to the emergence of drug resistance, pesticide residue and environmental contamination, it is important to develop novel eco-friendly strategies to protect plants. read more here.

Keywords: pyridazinone derivatives; novel plant; plant activators; new scaffold ... See more keywords

Natural and synthetic flavonoid derivatives as new potential tyrosinase inhibitors: a systematic review

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0 Published in 2021 at "RSC Advances"

DOI: 10.1039/d1ra03196a

Abstract: This review revealed that among all the natural and synthetic flavonoids, the inhibitory findings suggest that the flavonol moiety can serve as an effective and a lead structural scaffold for the further development of novel… read more here.

Keywords: natural synthetic; synthetic flavonoid; new potential; review ... See more keywords