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A novel megestrol acetate electrochemical sensor based on conducting functionalized acetylene black-CeO2NPs nanohybrids decorated glassy carbon microspheres.

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For the first time, megestrol acetate (MGA), a synthetic progestin with therapeutic use in breast cancer, is electrochemically studied to propose a new electroanalytical alternative for its detection in real samples. In the present work, a novel electrochemical sensor based on functionalized

5-Alkynyl-2'-deoxyuridines: chromatography-free synthesis and cytotoxicity evaluation against human breast cancer cells.

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Starting with 5-iodo-2'-deoxyuridine, a series of 5-alkynyl-2'-deoxyuridines (with n-propyl, cyclopropyl, 1-hydroxycyclohexyl, p-tolyl, p-tert-butylphenyl, p-pentylphenyl, and trimethylsilyl alkyne substituents) have been synthesized via the palladium-catalyzed (Sonogashira) coupling reaction

Functionalization of Cellulose Nanocrystals with POEGMA Copolymers via Copper-Catalyzed Azide-Alkyne Cycloaddition for Potential Drug-Delivery Applications.

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Elongated colloidal nanoparticles (NPs) have significant potential for drug delivery and imaging applications in cancer therapy, but progress depends on developing a deeper understanding of how their physicochemical properties affect their interactions with cells and with tumors. Cellulose

Novel 2,3-Dihydro-1H-pyrrolo[3,2,1-ij]quinazolin-1-ones: Synthesis and Biological Evaluation.

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Herein we describe the synthesis and evaluation of a series of novel 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinazolin-1-ones for in vitro cytotoxicity against three human cancer cell lines as well as for potential antimalarial activity against the chloroquine-sensitive strain 3D7 of Plasmodium falciparum.

Direct and nondestructive verification of PNA immobilization using click chemistry.

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The fluorogenic 1,3-Huisgen dipolar cycloaddition reaction was used as part of a novel immobilization strategy of PNA capture probes on a microarray. By using this click chemistry, azidocoumarin-anchored PNA probes were immobilized on phenyl acetylene-modified glass slides with the simultaneous

The synthesis and evaluation of a solution phase indexed combinatorial library of non-natural polyenes for reversal of P-glycoprotein mediated multidrug resistance.

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A combinatorial library of polyenes, based on (-)-stipiamide, has been constructed and evaluated for the discovery of new multidrug resistance reversal agents. A palladium coupling was used to react each individual vinyl iodide with a mixture of the seven acetylenes at near 1:1 stoichiometry. The

Intrabreath analysis of carbon monoxide uptake during exercise in patients at risk for lung injury.

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The single exhalation analysis of carbon monoxide, acetylene, and methane allows the determination of intrabreath (regional) DL, pulmonary capillary blood flow and ventilation inhomogeneities during rest and exercise. We reasoned that this technique might be more sensitive in detecting regional

Radioiodinated progesterone derivative for progesterone receptor targeting with enhanced nucleus uptake via phenylboronic acid conjugation.

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A novel ¹³¹ I-radiolabeled probe with aromatic boronate motif (¹³¹ I-EIPBA) was designed to target progesterone receptor (PR)-positive breast cancer with enhanced nucleus uptake. Acetylene progesterone was conjugated with pegylated phenylboronic acid via click reaction and

[Cyclopentadienyl]metalcarbonyl complexes of acetylsalicylic acid as neo-anticancer agents.

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[(Prop-2-ynyl)-2-acetoxybenzoate]dicobalthexacarbonyl (Co-ASS), a derivative of the nonsteroidal anti-inflammatory drug aspirin(®) (ASS), demonstrated high cytotoxic potential against various tumor cells. The [acetylene]Co(2)(CO)(6) cluster strongly increased the biological effects compared to

Polylactide-graft-doxorubicin nanoparticles with precisely controlled drug loading for pH-triggered drug delivery.

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Nanoparticles (NPs) with high drug loading and pH-responsivity were prepared by nanoprecipitation of a hydrophobic polymer-drug conjugate (PDC). The PDC, polylactide-graft-doxorubicin (PLA-g-DOX), was synthesized by azide-alkyne click reaction to transform acetylene-functionalized PLA into

Facile synthesis of chrysin-derivatives with promising activities as aromatase inhibitors.

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Flavones such as chrysin show structural similarities to androgens, the substrates of human aromatase, which converts androgens to estrogens. Aromatase is a key target in the treatment of hormone-dependent tumors, including breast cancer. Flavone-based aromatase inhibitors are of growing interest,

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