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Organic Radical Contrast Agents Based on Polyacetylenes Containing 2,2,6,6-Tetramethylpiperidine 1-Oxyl (TEMPO): Targeted Magnetic Resonance (MR)/Optical Bimodal Imaging of Folate Receptor Expressing HeLa Tumors in Vitro and in Vivo(a).
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Nitroxides have great potential as magnetic resonance imaging (MRI) contrast agents for tumor detection. Polyacetylenes(PAs) containing 2,2,6,6-tetramethyl-piperidine oxyl (TEMPO) and poly(ethylene glycol) were synthesized via metathesis polymerization of the corresponding substituted acetylenes to
Graphdiyne Nanosheet-Based Drug Delivery Platform for Photothermal/Chemotherapy Combination Treatment of Cancer.
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Nowadays, two-dimensional (2D) materials have attracted extensive attention as cancer drug delivery platforms owing to their unparalleled physicochemical properties and superior specific surface area. Graphdiyne (GDY) is a novel 2D carbon material. Compared with graphene, GDY not only has benzene
Electrochemical detection of anticancer drug topotecan using nano-acetylene black film.
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Topotecan, a novel anticancer drug, has been widely used in the treatment of ovarian and cervical cancers. Herein, acetylene black (AB) nanoparticles were used to modify the electrode surface, and the electrochemical behavior of topotecan was examined. At the AB film surface, an irreversible
Anti-cancer gold(I) phosphine complexes: Cyclic trimers and tetramers containing the P-Au-P moiety.
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We report the application of cationic tri- and tetra-nuclear gold(I) phosphine complexes [Au3(μ-dppen)3]X3 and [Au4(μ-dppa)4]X4 (X=OTf, PF6) [OTf=trifluoromethanesulfonate, dppen=trans-1,2-bis(diphenylphosphino)ethene, dppa=bis(diphenylphosphino)acetylene] for cancer treatment. The results of
Design, synthesis and biological evaluation of nonsecosteroidal vitamin D3 receptor ligands as anti-tumor agents.
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1α,25-dihydroxyvitamin D3 (1,25-(OH)2D3, also known as calcitriol), the active form of vitamin D3, is being increasingly recognized for cancer therapy. Our previous work showed that phenyl-pyrrolyl pentane analogs, which mimicked anti-proliferative activities against several cancer cell lines of the
Metabolite characterization of a novel anti-cancer agent, icotinib, in humans through liquid chromatography/quadrupole time-of-flight tandem mass spectrometry.
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Icotinib is a novel anti-cancer drug that has shown promising clinical efficacy and safety in patients with non-small-cell lung cancer (NSCLC). At this time, the metabolic fate of icotinib in humans is unknown. In the present study, a liquid chromatography/quadrupole time-of-flight tandem mass
Novel PIKK inhibitor antibody-drug conjugates: Synthesis and anti-tumor activity.
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Novel neolymphostin-based antibody-drug conjugate (ADC) precursors were synthesized either through amide couplings between both cleavable and non-cleavable linkers and neolymphostin derivatives, or through Cu(I)-catalyzed acetylene-azide click cycloadditon between non-cleavable linkers and
Hydrothiolation of benzyl mercaptan to arylacetylene: application to the synthesis of (E) and (Z)-isomers of ON 01910·Na (Rigosertib®), a phase III clinical stage anti-cancer agent.
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A stereoselective and efficient method for free radical addition of benzyl thiol to aryl acetylene in the presence of Et3B-hexane has been developed for the synthesis of (Z) and (E)-styryl benzyl sulfides where base catalyzed hydrothiolations have failed. The scope of this reaction was successfully
Core-shell structured upconversion nanocrystal-dendrimer composite as a carrier for mitochondria targeting and catalase enhanced anti-cancer photodynamic therapy.
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Recently, photodynamic therapy (PDT) has been deemed to be the most promising strategy for cancer treatment. To improve the efficacy for PDT, nanocarriers are expected to target mitochondria that are vulnerable to toxic reactive oxygen species (ROS). Moreover, overcoming tumor hypoxia is also
Intracellular DNA damage by lysine-acetylene conjugates.
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Previously, we reported the design and properties of alkyne C-lysine conjugates, a powerful and tunable family of DNA cleaving reagents. We also reported that, upon photoactivation, these molecules are capable of inducing cancer cells death. To prove that the cell death stems from DNA cleavage by
Compounds from the marine sponge Cribrochalina vasculum offer a way to target IGF-1R mediated signaling in tumor cells.
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In this work two acetylene alcohols, compound 1 and compound 2, which were isolated and identified from the sponge Cribrochalina vasculum, and which showed anti-tumor effects were further studied with respect to targets and action mechanisms. Gene expression analyses suggested insulin like growth
Design, synthesis, anticancer, antimicrobial activities and molecular docking studies of theophylline containing acetylenes and theophylline containing 1,2,3-triazoles with variant nucleoside derivatives.
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A new series of theophylline containing acetylene derivatives (6a-6b and 7-13) and theophylline containing 1,2,3-triazoles with variant nucleoside derivatives (20-32) have been designed and synthesized. These compounds were screened for anticancer and antimicrobial activity. Further the
3-Amino-8-hydroxy-4-imino-6-methyl-5-phenyl-4,5-dihydro-3H-chromeno [2,3-d]pyrimidine: an effecient key precursor for novel synthesis of some interesting triazines and triazepines as potential anti-tumor agents.
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A number of interesting heterocycles were prepared through interaction of the intermediate 3-amino-8-hydroxy-4-imino-6-methyl-5-phenyl-4,5-dihydro-3H-chromeno-[2,3-d]pyrimidine (1) and reagents such as hydrazonyl halides 2 to furnish triazine derivatives 4a-l. Reaction of 1 with phenacyl bromide
Cytotoxic activity of polyacetylenes and polyenes isolated from roots of Echinacea pallida.
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OBJECTIVE
The n-hexane extracts of the roots of three medicinally used Echinacea species exhibited cytotoxic activity on human cancer cell lines, with Echinacea pallida found to be the most cytotoxic. Acetylenes are present in E. pallida lipophilic extracts but essentially absent in extracts from
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.
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