Results 141 to 150 of about 145,419 (376)

Synthesis of Siphonazole B Through Domino Cycloisomerization‐Oxazolonium Ion Rearrangements

open access: yesChemistry – A European Journal, EarlyView.
The study by Strand and co‐workers describes a concise synthesis of siphonazole B. Both oxazole units are formed from a simple propargylamine using a novel domino cycloisomerization‐rearrangement approach. Additional synthetic features include a direct aldol‐type reaction for assembling the tricyclic siphonazole core and an oxidative amidation reaction
Filip Paulsen   +5 more
wiley   +1 more source

Functionalized in Triplicate: A Ring‐By‐Ring Approach to Tailored Prodiginine Derivatives for Site‐Specific Conjugation Through Click Chemistry

open access: yesChemistry – A European Journal, EarlyView.
Prodigiosin is a potent cytotoxic alkaloid but lacks target selectivity. We advance functionalization of all three pyrrole rings of prodigiosin to enable site‐specific conjugation via click chemistry. The presented azide‐ and maleimide‐functionalized prodiginines are suitable for generating covalent prodiginine conjugates and attaching auspicious ...
T. Moritz Weber, Jörg Pietruszka
wiley   +1 more source

Targeting Ubiquitin‐Specific Protease 7 with Novel 5‐Amino‐Pyrazole Inhibitors: Design, Synthesis, and Biological Evaluation

open access: yesChemMedChem, EarlyView.
Ubiquitin‐specific protease 7 (USP‐7) is a novel target for anticancer therapy. To further extend the structure–activity relationships of the previously USP‐7 inhibitor STIRUR‐41, a library of 5‐aminopyrazoles is reported. 1d shows a potency comparable to lead compound STIRUR‐41 and promising in silico and in vitro pharmacokinetic properties ...
Matteo Lusardi   +9 more
wiley   +1 more source

Antidepressants versus placebo for depression in primary care [PDF]

open access: yes, 2009
Arroll, Bruce   +7 more
core   +2 more sources

Beyond Docking: A Multitier Computational Pipeline for USP7 Inhibitor Optimization

open access: yesChemMedChem, EarlyView.
A multitier computational strategy discovers potential USP7 inhibitors using similarity‐based virtual screening, physics‐driven molecular simulations, binding free energy estimations, binary QSAR modeling, and steered molecular dynamics analysis. This integrated approach prioritizes and optimizes lead compounds with strong predicted affinity, offering ...
Ehsan Sayyah   +2 more
wiley   +1 more source

The Role of Five‐Membered Aromatic Rings Containing N and O in Modulating Bile Acid Receptors: An Overview

open access: yesChemMedChem, EarlyView.
Several derivatives incorporating five‐membered aromatic rings are described in this review as bile acid receptor modulators, particularly targeting the farnesoid X receptor and the G protein‐coupled bile acid receptor 1. This review provides a comprehensive analysis of patents and literature that is useful to support researchers in the design of new ...
Claudia Finamore   +5 more
wiley   +1 more source

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