New indole based hybrid oxadiazole scaffolds with N-substituted acetamides: As potent anti-diabetic agents.
Sign Up to like & getrecommendations! Published in 2018 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.08.010
Abstract: Current study is based on the sequential conversion of indolyl butanoic acid (1) into ethyl indolyl butanoate (2), indolyl butanohydrazide (3), and 1,3,4-oxadiazole-2-thiol analogs (4) by adopting chemical transformations. In a parallel series of reactions,… read more here.
Keywords: oxadiazole scaffolds; hybrid oxadiazole; scaffolds substituted; based hybrid ... 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
Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113893
Abstract: The equilibrium between histone acetylation and deacetylation plays an important role in cancer initiation and progression. The histone deacetylases (HDACs) are a class of key regulators of gene expression that enzymatically remove an acetyl moiety… read more here.
Keywords: based hydroxamic; design synthesis; hydroxamic acid; acid derivatives ... See more keywords
Identification of indole-based activators of insulin degrading enzyme.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113982
Abstract: Insulin degrading enzyme (IDE) is a zinc metalloprotease that cleaves numerous substrates among which amyloid-β and insulin. It has been linked through genetic studies to the risk of type-2 diabetes (T2D) or Alzheimer's disease (AD).… read more here.
Keywords: identification indole; degrading enzyme; insulin degrading; activators insulin ... See more keywords
Indole-based fluorescence sensors for both cations and anions
Sign Up to like & getrecommendations! Published in 2018 at "Inorganica Chimica Acta"
DOI: 10.1016/j.ica.2018.06.023
Abstract: Abstract The fluorescence properties of the ligand idpa (1H-Indole-3-ethanamine, N,N-bis(2-pyridinylmethyl)amine) complexed with metal ions along with their crystal structures were investigated to further understand the role of π contacts in quenching fluorescence. In particular, the… read more here.
Keywords: state; idpa; fluorescence; indole based ... See more keywords
Exploring efficacy of indole-based dual inhibitors for α-glucosidase and α-amylase enzymes: In silico, biochemical and kinetic studies.
Sign Up to like & getrecommendations! Published in 2020 at "International journal of biological macromolecules"
DOI: 10.1016/j.ijbiomac.2020.03.090
Abstract: α-Glucosidase and α-amylase are enzymes which are associated with diabetic II. These enzymes break macromolecules of sugar into monosugar molecules which is soluble in body, hence increase the sugar level in blood. There is need… read more here.
Keywords: exploring efficacy; glucosidase amylase; amylase enzymes; efficacy indole ... See more keywords
QSAR and molecular docking studies of indole-based analogs as HIV-1 attachment inhibitors
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Molecular Structure"
DOI: 10.1016/j.molstruc.2019.05.056
Abstract: Abstract Human immunodeficiency virus-1 (HIV-1) glycoprotein 120 (gp120) is one of the key targets for treatment of acquired immunodeficiency syndrome. A large number of inhibitors are being designed for this target in order to find… read more here.
Keywords: attachment inhibitors; qsar molecular; indole based; molecular docking ... See more keywords
Indole-based alkaloids from Ophiocordyceps xuefengensis.
Sign Up to like & getrecommendations! Published in 2020 at "Phytochemistry"
DOI: 10.1016/j.phytochem.2020.112536
Abstract: Seven undescribed indole-based alkaloids, xuefengins A-D and xuefenglasins A-C, were isolated from natural Ophiocordyceps xuefengensis, along with six known alkaloids. Their structures were elucidated by comprehensive spectroscopy, with absolute configurations confirmed by comparison with calculated… read more here.
Keywords: ophiocordyceps xuefengensis; based alkaloids; spectroscopy; alkaloids ophiocordyceps ... See more keywords
New chiral ferrocene/indole-based diphosphine ligands for Rh-catalyzed asymmetric hydrogenation of functionalized olefins
Sign Up to like & getrecommendations! Published in 2020 at "Tetrahedron Letters"
DOI: 10.1016/j.tetlet.2020.151860
Abstract: Abstract Convenient synthesis of a new family of chiral ferrocene/indole-based diphosphine ligands, (Rc,Rp)-IndoFerroPhos (L), from (Sc,Rp)-PPFA and 2-(diphenylphosphino)indole has been described. These new ligands exhibited high efficiency in the Rh-catalyzed asymmetric hydrogenation of functionalized olefins… read more here.
Keywords: diphosphine ligands; based diphosphine; chiral ferrocene; indole ... See more keywords
Synthesis, molecular docking simulation and enzymatic degradation of AB-type indole-based polyesters with improved thermal properties.
Sign Up to like & getrecommendations! Published in 2020 at "Biomacromolecules"
DOI: 10.1021/acs.biomac.9b01399
Abstract: We report the facile synthesis of a series of indole-based hydroxyl-carboxylate (AB-type) monomers by a one-step procedure. These monomers were successfully polymerized by melt-polycondensation to yield AB-type polyesters with a varied number of flexible methylene… read more here.
Keywords: degradation; based polyesters; type; molecular docking ... See more keywords
Synthesis and Anticancer Evaluation of Novel Indole Based Arylsulfonylhydrazides against Human Breast Cancer Cells
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.2c03908
Abstract: A series of novel indole based sulfonohydrazide derivatives (5a–k) containing morpholine heterocyclic ring were synthesized through multistep chemical reactions. The target compounds (5a–k) were prepared by the reaction of substituted phenyl sulfonylhydrazides (2a–k) with morpholine… read more here.
Keywords: breast cancer; novel indole; cancer; indole based ... See more keywords