18 research outputs found

    2,2′-Diazinodimethylidyne)di-o-phenyl­ene) dibenzoate

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    The title compound, C28H20N2O4, was synthesized by the reaction of 2-(hydrazonometh­yl)phenyl benzoate with iodine. The mol­ecule possesses a crystallographically imposed center of symmetry at the mid-point of the hydrazine N—N bond. The substituents at the ends of the C=N bonds adopt an E,E configuration. Inter­molecular C—H⋯π(arene) hydrogen bonds and aromatic π–π stacking inter­actions [centroid–centroid distance 3.900 (1) Å] link the mol­ecules into (100) sheets. In addition, there is an inter­molecular C—H⋯O hydrogen-bond inter­action

    Design, synthesis and bioactivity of catechin/epicatechin and 2-azetidinone derived chimeric molecules

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    A new class of chimeric molecules have been developed. These are based on polyphenols like catechin and epicatechin and monocyclic β-lactams. The two units are joined via a triazole linker using the 'Click Chemistry' conditions. The compounds showed good to weak antibacterial activity against Escherichia coli as well as moderate inhibition of RNase A

    Advancement in Biopolymer Assisted Cancer Theranostics

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    Applications of nanotechnology have increased the importance of research and nanocarriers, which have revolutionized the method of drug delivery to treat several diseases, including cancer, in the past few years. Cancer, one of the world’s fatal diseases, has drawn scientists’ attention for its multidrug resistance to various chemotherapeutic drugs. To minimize the side effects of chemotherapeutic agents on healthy cells and to develop technological advancement in drug delivery systems, scientists have developed an alternative approach to delivering chemotherapeutic drugs at the targeted site by integrating it inside the nanocarriers like synthetic polymers, nanotubes, micelles, dendrimers, magnetic nanoparticles, quantum dots (QDs), lipid nanoparticles, nano-biopolymeric substances, etc., which has shown promising results in both preclinical and clinical trials of cancer management. Besides that, nanocarriers, especially biopolymeric nanoparticles, have received much attention from researchers due to their cost-effectiveness, biodegradability, treatment efficacy, and ability to target drug delivery by crossing the blood-brain barrier. This review emphasizes the fabrication processes, the therapeutic and theragnostic applications, and the importance of different biopolymeric nanocarriers in targeting cancer both in vitro and in vivo, which conclude with the challenges and opportunities of future exploration using biopolymeric nanocarriers in onco-therapy with improved availability and reduced toxicity. © 2023 The Authors. Published by American Chemical Society.TRU

    Mechanism of Alcohol Oxidation by Fe<sup>V</sup>(O) at Room Temperature

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    Selective oxidation of alcohol to its corresponding carbonyl compound is an important chemical process in biological as well as industrial reactions. The heme containing enzyme CytP450 has been known to selectively oxidize alcohols to their corresponding carbonyl compounds. The mechanism of this reaction, which involves high-valent Fe<sup>IV</sup>(O)−porphyrin<sup>•+</sup> intermediate with alcohol, has been well-studied extensively both with the native enzyme and with model complexes. In this paper, we report for the first time the mechanistic insight of alcohol oxidation with Fe<sup>V</sup>(O) complex of biuret TAML (bTAML), which is isoelectronic with Fe<sup>IV</sup>(O)−porphyrin<sup>•+</sup> intermediate form in CytP450. The oxidations displayed saturation kinetics, which allowed us to determine both the binding constants and first-order rate constants for the reaction. The <i>K</i> and <i>k</i> values observed for the oxidation of benzyl alcohol by Fe<sup>V</sup>(O) at room temperature (<i>K</i> = 300 M<sup>–1</sup>, <i>k</i> = 0.35 s<sup>–1</sup>) is very similar to that obtained by CytP450 compound I at −50 °C (<i>K</i> = 214 M<sup>–1</sup>, <i>k</i> = 0.48 s<sup>–1</sup>). Thermodynamic parameters determined from van’t Hoff’s plot (Δ<i>H</i>∼ −4 kcal/mol) suggest hydrogen bonding interaction between substrate and bTAML ligand framework of the Fe<sup>V</sup>(O) complex. Analysis of H/D KIE (<i>k</i><sub>H</sub>/<i>k</i><sub>D</sub> ∼ 19 at 303 K), Hammett correlation and linearity in Bell-Evans-Polyanski plot points to the C–H abstraction as the rate determination step. Finally, experiments using Fe<sup>V</sup>(O<sup>18</sup>) for benzyl alcohol oxidation and use of the “radical clock” cyclobutanol as a substrate shows the absence of a rebound mechanism as is observed for CytP450. Instead, an ET/PT process is proposed after C–H abstraction leading to formation of the aldehyde, similar to what has been proposed for the heme and nonheme model compounds

    Advancement in biopolymer assisted cancer theranostics

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    Applications of nanotechnology have increased the importance of research and nanocarriers, which have revolutionized the method of drug delivery to treat several diseases, including cancer, in the past few years. Cancer, one of the world’s fatal diseases, has drawn scientists’ attention for its multidrug resistance to various chemotherapeutic drugs. To minimize the side effects of chemotherapeutic agents on healthy cells and to develop technological advancement in drug delivery systems, scientists have developed an alternative approach to delivering chemotherapeutic drugs at the targeted site by integrating it inside the nanocarriers like synthetic polymers, nanotubes, micelles, dendrimers, magnetic nanoparticles, quantum dots (QDs), lipid nanoparticles, nano-biopolymeric substances, etc., which has shown promising results in both preclinical and clinical trials of cancer management. Besides that, nanocarriers, especially biopolymeric nanoparticles, have received much attention from researchers due to their cost-effectiveness, biodegradability, treatment efficacy, and ability to target drug delivery by crossing the blood−brain barrier. This review emphasizes the fabrication processes, the therapeutic and theragnostic applications, and the importance of different biopolymeric nanocarriers in targeting cancer both in vitro and in vivo, which conclude with the challenges and opportunities of future exploration using biopolymeric nanocarriers in onco-therapy with improved availability and reduced toxicity</p
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