Results 81 to 90 of about 48,200 (259)

New Quinoline-Based Heterocycles as Anticancer Agents Targeting Bcl-2

open access: yesMolecules, 2019
The Bcl-2 protein has been studied as an anticancer drug target in recent years, due to its gatekeeper role in resisting programmed cancer cell death (apoptosis), and the design of BH3 domain mimetics has led to the clinical approval of Venetoclax (ABT ...
Rania Hamdy   +4 more
doaj   +1 more source

Synthesis of 1,2,3-triazoles and applications in the synthesis of BODIPY triazoles

open access: yes, 2020
The 1,2,3-triazole ring is an important heterocycle which has found wide applications due to its interesting properties. Mainly due to the advent of the copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction, 1,2,3-triazoles are nowadays unavoidable in the chemical literature. In the past decade, the development of transition metal-free synthetic
openaire   +2 more sources

Toward Chromoselective Transformations in Biological Systems: Perspectives and Challenges

open access: yesAngewandte Chemie International Edition, EarlyView.
Controlling biological systems with small‐molecule chromophores has evolved into a powerful strategy and is applied from chemical biology to medicine. However, the complexity of in vivo systems cannot be matched by a single wavelength of light. Developing methods to combine and individually control multiple chromophores is crucial.
Nadja A. Simeth
wiley   +1 more source

Unlocking Catalyst Activation as a Critical Bottleneck in Cross‐Coupling Reactions: Room‐Temperature Couplings of Weak Nucleophiles Enabled by [Pd(1‐MeNAP)TFA]2 Precatalysts

open access: yesAngewandte Chemie International Edition, EarlyView.
In many Pd‐catalyzed cross‐couplings, catalyst performance has been found to be limited by catalyst activation. Methylnaphthyl (MeNAP) palladium trifluoroacetate dimers are presented as easy‐to‐store and easy‐to‐handle precursors, which rapidly activate under reaction conditions, even when only weakly coordinating, non‐reducing nucleophiles are present.
Sourav Manna   +6 more
wiley   +1 more source

9-Ethyl-6-methyl-7H-1,2,4-triazolo[4,3-b][1,2,4]triazepin-8(9H)-one

open access: yesIUCrData, 2016
In the title compound, C8H11N5O, the triazepine ring displays a boat conformation. Its mean plane is inclined to the triazole ring by 22.10 (9)°. In the crystal, molecules are linked by C—H...O hydrogen bonds to form chains parallel to the b-axis ...
Youness El Bakri   +4 more
doaj   +1 more source

Late‐Stage Functionalization of Peptides on the Solid Phase

open access: yesAngewandte Chemie International Edition, EarlyView.
Peptide modifications are essential to control pharmacodynamic and pharmacokinetic properties of peptide drugs. Consequently, strategies that allow for efficient and rapid incorporation of non‐canonical modifications into peptides in parallel formats are highly sought after.
Marius Werner   +2 more
wiley   +1 more source

Synthesis and physical-chemical properties of 6-(5-(1Н-tetrazole-1-ylmethyl)-4-R-1,2,4-triazole-3-ylthio)pyridin-3-amines and 6-((5-(1Н-tetrazole-1-yl)methil-4-R-1,2,4-triazole-3-ylthio)pyridin-3-yl)-(alk,ar,heter)ylmethanimines

open access: yesZaporožskij Medicinskij Žurnal, 2017
Over the past decade the number of publications, that contain different aspects of chemistry and use of triazoles and tetrazoles have been doubled and continues to grow. Puplications of recent years show that heterocycles with 1,2,3,4-teterazoles and 1,2,
Yu. S. Hulina, A. G. Kaplaushenko
doaj   +1 more source

Syntheses, Antibacterial and Antifungal Activities of Substituted-Thiazolo-1,3,4-Thiadiazoles, 1,3,4-Oxadiazoles and 1,2,4-Thiazoles [PDF]

open access: yesIranian Journal of Chemistry & Chemical Engineering, 1998
Starting from readily available 2-substituted-4-methylthiazole-5-carboxylic acid hydrazide (1), The title compounds were prepared. The reaction of compound 1 (R=CH3) with formic acid yielded 1-(formyl)-2-(2,4-dimethylthiazole-5-carboxyl) hydrazine (2 ...
Abbas Shafiee   +2 more
doaj  

Use of Clotrimazole in Finfish Aquaculture: Mechanistic Insights, Limitations, and Future Directions for Antifungal Therapy

open access: yesAnimal Research and One Health, EarlyView.
This review critically evaluates clotrimazole as a potential antifungal for finfish aquaculture, highlighting strong mechanistic and in vitro efficacy against aquatic mycoses alongside major gaps in in vivo evidence, toxicokinetics, residue safety, and environmental risk, outlining priorities for responsible therapeutic development and regulatory ...
Arya Sen   +2 more
wiley   +1 more source

Discovery of CRBN‐based molecular glue degraders targeting WIZ transcription factor

open access: yesBulletin of the Korean Chemical Society, EarlyView.
This work reports the discovery of 9l, a novel cereblon‐based molecular glue degrader which targets the WIZ transcription factor. Compound 9l facilitates WIZ‐CRBN ternary complex formation to degrade WIZ, subsequently inducing γ‐globin expression in HUDEP‐2 cells and highlighting its potential as a sickle cell disease therapy.
Tae‐Jun Kim   +8 more
wiley   +1 more source

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