3-Bromo-6-nitro-1-(prop-2-yn­yl)-1H-indazole

In the title compound, C10H6BrN3O2, the indazole fused-ring system is nearly planar (r.m.s. deviation = 0.008 Å); its nitro substituent is nearly coplanar with the fused ring [dihedral angle = 4.5 (2)°]. In the crystal, adjacent mol­ecules are linked by weak acetyl­ene–nitro C—H⋯O hydrogen bonds, generating a helical chain running along the b axis

1-Allyl-3-chloro-6-nitro-1H-indazole

The indazole system in each of the two independent mol­ecules of the title compound, C10H8ClN3O2, is planar (r.m.s. deviations = 0.005 and 0.005 Å). The nitro group is coplanar with the fused-ring system [dihedral angles = 1.3 (3) and 4.8 (3) Å]

An overview on the synthesis and anticancer properties of ethacrynic acid and their analogues

Ethacrynic acid (EA, Edecrin) is a well-known diuretic drug used in the treatment of high blood pressure and the swelling caused by diseases such as congestive heart failure, liver failure, and kidney failure. EA has an α,β-unsaturated carbonyl unit which acts as a Michael acceptor involved in the inhibition of the major classes of glutathione S-transferases (GSTs) (α, μ, and π) that plays a crucial role in regulating the multidrug resistance. Moreover, EA was used as an adjuvant to improve the therapeutic efficacy of several anticancer chemotherapeutic agents. EA and their derivatives have received considerable attention in the past decades due to their interesting biological properties. This review highlights the recent development in this area, focusing on their synthesis and their antitumor activities

Unlocking the Potential of Deep Eutectic Solvents for C–H Activation and Cross-Coupling Reactions: A Review

Green chemistry principles have underpinned the development of deep eutectic solvents (DESs). In this brief overview, we discuss the potential of DESs as a greener alternative to volatile organic solvents for cross-coupling and C–H activation reactions in organic chemistry. DESs offer numerous benefits, such as easy preparation, low toxicity, high biodegradability, and the potential to replace volatile organic compounds. The ability of DESs to recover the catalyst-solvent system enhances their sustainability. This review highlights recent advances and challenges in utilizing DESs as a reaction media, as well as the impact of physicochemical properties on the reaction process. Several types of reactions are studied to highlight their effectiveness at promoting C–C bond formation. Aside from demonstrating the success of DESs in this context, this review also discusses the limitations and future prospects of DESs in organic chemistry

First-in-class combination therapy of a copper(II) metallo-phosphorus dendrimer with cytotoxic agents

International audienceThe metallo-phosphorus dendrimer 1G3-Cu (generation 3 dendrimer bearing 48 conjugated copper(II) on its surface) has antiproliferative activity related to its capacity to activate Bax translocation. In the present study, we evaluate the activity of an association of 1G3-Cu with 5 cytotoxic agents used in chemotherapy having different modes of action. Data show no additive effect with camptothecin and cisplatin, additivity with paclitaxel and MG132, and synergy with doxorubicin. Results suggest that the multivalent Cu-conjugated dendrimer 1G3-Cu (activator of Bax translocation) plays an important role in boosting the clinical impact of Bax accumulation stimulated by the proteasome inhibitor MG132, antimitotic taxanes, and the topo II inhibitor doxorubicin

Orthogonal synthesis of covalent polydendrimer frameworks by fusing classical and onion-peel phosphorus-based dendritic units

International audienceWe report novel and new giant three-dimensional polymers having dendrimers as repeating units. The approach is illustrated here for macromolecular synthesis by polymeric condensation of well-defined single phosphorus dendrimers units. Specifically, classical and onion-peel phosphorus dendrimers, constructed by a divergent method from a cyclotriphosphazene core, were fused within the same tectonic nanostructure by several polymeric condensation approaches including hydrazine-to-aldehyde Schiff-base formation and amine-to carboxylic acid peptide-like coupling. These reticular, easy to run metal free routes afford a new library of hyperbranched macromolecular materials, featuring various phosphorus layers (both alternated and dissymmetrical), well-defined textured nanospheres, and controllable nanometric ordered substructures. The scope of the concept is successfully expanded to the integration of electro-redox viologen units resulting in the synthesis of new photoactive macromolecular materials

Synthesis and evaluation of a novel class of ethacrynic acid derivatives containing triazoles as potent anticancer agents

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Copper complexes of phosphorus dendrimers and their properties

International audiencePhosphorus dendrimers are highly branched macromolecules, built with one phosphorus atom at each branching point. These dendrimers can be functionalized at will on the terminal functions. Grafting as terminal functions ligands suitable for the complexation of copper has been carried out several times, in particular with the aim of using the corresponding complexes as catalysts in a range of reactions, from O-and N-arylations and-vinylations, to the asymmetric benzoylation of linear or cyclic diols. A sequel of this work concerns the study of anticancer activity of analogous dendritic copper complexes