Results 91 to 100 of about 12,506 (227)

Synthesis and Biological Evaluation of Well‐Defined M6P(n)‐Modified Glycopeptides for Targeted Protein Degradation

open access: yesChemistry – A European Journal, Volume 32, Issue 33, 1 September 2026.
A synthetic methodology has been developed to prepare multifunctional M6P and M6Pn ligands of different valency. The glycopeptides were conjugated to cetuximab and then examined to mediate cellular uptake of fluorescently labeled EGFRvIII. Only cetuximab modified by glycopeptides having 3 or 6 M6P or M6Pn residues demonstrated greater uptake.
Patrycja Lenartowicz   +6 more
wiley   +1 more source

Dehydroabietylamine derived bistetrazoles from ultrasound-assisted pseudo-seven-component Ugi reactions act as efficient and selective inhibitors of cholinesterases

open access: yesEuropean Journal of Medicinal Chemistry Reports
The reaction of dehydroabiethylamine (DHA) with isocyanides and formaldehyde produces varying products depending on the conditions employed. In a 4-component Ugi reaction using benzyl isocyanide, paraformaldehyde, and TMS-azide, the anticipated tetrazole
Niels V. Heise   +3 more
doaj   +1 more source

Concise Synthesis of Tetrazole-Ketopiperazines by Two Consecutive Ugi Reactions [PDF]

open access: yes, 2015
A concise route for the synthesis of the novel compound class tetrazole-diketopiperazines was developed. The approach involves the use of two multicomponent reactions: the Ugi tetrazole four-component reaction (4CR) and the classical intramolecular Ugi ...
Patil, Pravin   +5 more
core   +2 more sources

Investigation of the In Vitro and In Silico Anticancer Potential of Novel 4‐Arylthiazole‐Hydrazone Derivatives

open access: yesChemical Biology &Drug Design, Volume 108, Issue 3, September 2026.
The synthesized compounds exhibited excellent cytotoxicity on MCF‐7, breast cancer cell line with selective profile especially 2d with IC50 value of 0.12 μM. Three compounds 2c, 2d, and 2h caused almost as much apoptosis induction as cisplatin. Compound 2d exhibited caspase‐3 activation at standard drug level.
Zeynep Zişan Demirci   +3 more
wiley   +1 more source

Targeting Human Immunodeficiency Virus Integrase Beyond the Active Site: The Discovery and Development of Allosteric Integrase Inhibitors

open access: yesChemMedChem, Volume 21, Issue 16, 27 August 2026.
Human immunodeficiency virus (HIV) allosteric integrase inhibitors (ALLINIs) offer a vital alternative to standard therapies by targeting noncatalytic sites. By inducing aberrant integrase multimerization, they disrupt viral maturation. This review explores their medicinal chemistry evolution, detailing structural insights, structure–activity ...
Francesco Saccoliti   +10 more
wiley   +1 more source

5-p-Tolyl-1H-tetrazole

open access: yes, 2009
The title compound, C8H8N4, possesses crystallographic mirror symmetry, with four C atoms lying on the reflecting plane, which bisects the phenyl and tetrazole rings. It is composed of a planar r.m.s.
Dong-Yue Hu, Zhi-Rong Qu, Xiao-Wei Chu
core   +1 more source

Structure‐Guided Optimization of a Molecular Glue Targeting the KBTBD4‐HDAC1/2 Complex

open access: yesChemMedChem, Volume 21, Issue 16, 27 August 2026.
Structure‐based optimization of the molecular glue degrader UM171 resulted in a near 20‐fold improvement of ternary complex stability but also revealed the challenges of glue discovery. Optimization of UM171, a molecular glue initiating the degradation of neosubstrate HDAC1/2–CoREST–LSD1 through a multiprotein complex formed with KBTBD4, was carried ...
Timea Balo   +8 more
wiley   +1 more source

Crystal structure of 4-methylsulfanyl-2-(2H-tetrazol-2-yl)pyrimidine

open access: yesActa Crystallographica Section E: Crystallographic Communications, 2015
The title compound, C6H6N6S, crystallized with two independent molecules (A and B) in the asymmetric unit. The conformation of the two molecules differs slightly.
Andreas Thomann   +2 more
doaj   +1 more source

Sulfonylurea Bioisosteres of Sulfonic Acid in JFD 00458‐Based ST6GAL1 Inhibitors Enhance Membrane Permeability

open access: yesChemMedChem, Volume 21, Issue 16, 27 August 2026.
ST6GAL1 sialylates glycoconjugates in the Golgi, modulating immune recognition and enabling tumor immune evasion. To effectively reach ST6GAL1, inhibitors should demonstrate good membrane permeability. Based on nonpermeable hit JFD 00458, we developed sulfonylurea analogs achieving increased membrane permeability and potency.
Natan Koraj   +9 more
wiley   +1 more source

Self-reporting fluorescent step-growth RAFT polymers based on nitrile imine-mediated tetrazole-ene cycloaddition chemistry

open access: yes, 2017
We introduce an inherently fluorescent self-reporting step-growth polymer system as well as a fluorescence-based methodology for accessing the kinetics of the underpinning photoinduced nitrile imine-mediated tetra-zole-ene cycloaddition (NITEC) process ...
Estupinan, Diego   +14 more
core   +1 more source

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