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Identification of 5-nitrofuran-2-amide derivatives that induce apoptosis in triple negative breast cancer cells by activating C/EBP-homologous protein expression.

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The transcription factor C/EBP-homologous protein (CHOP) is a key component of the terminal unfolded protein response (UPR) that mediates unresolvable endoplasmic reticulum stress-induced apoptosis. CHOP induction is known to cause cancer cell death. Chemicals that induce CHOP expression would thus

Amide proton transfer imaging of glioblastoma, neuroblastoma, and breast cancer cells on a 11.7 T magnetic resonance imaging system.

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The purpose of this study was (i) to determine the optimal magnetization transfer (MT) pulse parameter for amide proton transfer (APT) chemical exchange saturation transfer (CEST) imaging on an ultra-high-field magnetic resonance imaging (MRI) system and (ii) to use APT CEST imaging to

A natural piper-amide-like compound NED-135 exhibits a potent inhibitory effect on the invasive breast cancer cells.

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Invasiveness and metastasis are the primary factors indicating poor prognosis in breast cancer patients. To identify a novel lead compound for the development of therapeutics for the treatment of breast cancer through inhibiting invasion, we screened the natural piper amide-like compounds library

In vitro antitumor activity evaluation of some 1,2,4-triazine derivatives bearing piperazine amide moiety against breast cancer cells.

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A series of 1,2,4-triazine derivatives bearing piperazine amide moiety has been synthesized and investigated for their potential anticancer activities. 1-[4-(5,6-Bis(4-subtituted phenyl)-1,2,4-triazin-3-yl)piperazin-1-yl]-2-[4-(3-substituted phenyl)piperazin-1-yl]ethanone derivative (1-32) compounds

Synthesis of new 2-galactosylthiazolidine-4-carboxylic acid amides. Antitumor evaluation against melanoma and breast cancer cells.

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A set of 2-galactosylthiazolidine-4-carboxylic acid amides was synthesized with different length for the carbon chain amide moiety. The cytotoxicity of the molecules was evaluated against A375 melanoma and MCF7 breast cancer cell lines. For the derivatives tested, the one that contains a C(16) amide

Pharmacological explorations of eco-friendly amide substituted (Z)-β-enaminones as anti-breast cancer drugs.

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Amide substituted (Z)-β-enaminones were synthesized by green chemistry and stereo-specific synthetic pathway as novel phosphoinositide 3-kinase (PI3K) inhibitors and breast cancer drugs. PI3K inhibition was measured by competitive ELISA. A panel of cancer cell lines including MCF-7 (breast cancer),

Antitumor activity of raloxifene-targeted poly(styrene maleic acid)-poly (amide-ether-ester-imide) co-polymeric nanomicelles loaded with docetaxel in breast cancer-bearing mice.

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Purpose Raloxifene (RA) receptors have over-expressed GPER-positive breast cancer tumors. The purpose of this work was to evaluate the antitumor activity and pharmacokinetic behavior of docetaxel (DTX), loaded in RA-targeted nanomicelles, which were designed to overcome a lack of specific

A novel normalization for amide proton transfer CEST MRI to correct for fat signal-induced artifacts: application to human breast cancer imaging.

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The application of amide proton transfer (APT) CEST MRI for diagnosis of breast cancer is of emerging interest. However, APT imaging in the human breast is affected by the ubiquitous fat signal preventing a straightforward application of existing acquisition protocols. Although the

Synthesis And In Vitro/In Vivo Characterization Of Raloxifene Grafted Poly(Styrene Maleic Acid)-Poly (Amide-Ether-Ester-Imide¬¬) Micelles For Targeted Delivery Of Docetaxel In G Protein-Coupled Estrogen Receptor Breast Cancer.

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BACKGROUND To reduce the nonspecifically distribution of chemotherapeutic agents throughout the whole body, which causes severe toxicity in normal tissues, targeting them towards a receptor overexpressed on tumor tissue, is a promising method for cancer therapy. OBJECTIVE The aim of the present

Amide chemical exchange saturation transfer at 7 T: a possible biomarker for detecting early response to neoadjuvant chemotherapy in breast cancer patients.

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BACKGROUND The purpose of this work was to investigate noninvasive early detection of treatment response of breast cancer patients to neoadjuvant chemotherapy (NAC) using chemical exchange saturation transfer (CEST) measurements sensitive to amide proton transfer (APT) at 7 T. METHODS CEST images

Contradiction between amide-CEST signal and pH in breast cancer explained with metabolic MRI.

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Metabolic MRI is a noninvasive technique that can give new insights into understanding cancer metabolism and finding biomarkers to evaluate or monitor treatment plans. Using this technique, a previous study has shown an increase in pH during neoadjuvant chemotherapy (NAC) treatment,

Biosynthesis and degradation of bioactive fatty acid amides in human breast cancer and rat pheochromocytoma cells--implications for cell proliferation and differentiation.

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The endogenous cannabinoid, anandamide (arachidonoylethanolamide), and the sleep-inducing factor, oleamide (cis-9-octadecenoamide), represent two classes of long-chain fatty acid amides with several neuronal actions and metabolic pathways in common. Here we report that these two compounds are

Comparative Study of Amide Proton Transfer-Weighted Imaging and Intravoxel Incoherent Motion Imaging in Breast Cancer Diagnosis and Evaluation.

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Amide proton transfer-weighted imaging (APTWI) and intravoxel incoherent motion imaging (IVIM) are valuable MRI techniques applied to cancer.To compare APTWI and IVIM in the diagnosis of benign and malignant breast lesions and to evaluate the correlations

A comparative study of the value of amide proton transfer-weighted imaging and diffusion kurtosis imaging in the diagnosis and evaluation of breast cancer

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Objectives: To compare the value of amide proton transfer-weighted imaging (APTWI) and diffusion kurtosis imaging (DKI) in differentiating benign and malignant breast lesions and analyze the correlations between the derived parameters and

Inhibition of fatty acid amide hydrolase activates Nrf2 signalling and induces heme oxygenase 1 transcription in breast cancer cells.

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OBJECTIVE Endocannabinoids such as anandamide (AEA) are important lipid ligands regulating cell proliferation, differentiation and apoptosis. Their levels are regulated by hydrolase enzymes, the fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL). Here, we investigated whether FAAH

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