51 research outputs found

    Making cycles, bicycles and macrocycles

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    EThOS - Electronic Theses Online ServiceGBUnited Kingdo

    Targeted Protein Degradation

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    The Intermolecular Pauson—Khand Reaction

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    Die intermolekulare Pauson‐Khand‐Reaktion

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    La tomografia a emissione di positroni (PET) con F-18 FDG nello studio delle formazioni espansive a sede surrenalica: confronto tra lesioni benigne e maligne

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    In this study, 15 patients (4 men and 11 women, mean age: 50 +/- 13 years) with unilateral adrenal masses detected on ultrasound (US), Computed Tomography (CT) and/or Magnetic Resonance (MR) studies were submitted to positron emission tomography (PET) with fluorine-18 deoxyglucose (FDG). Histology demonstrated 3 adenomas, 1 myelolipoma, 1 angiolipoma, 1 neurinoma, 1 cyst, 1 malignant pheochromocytoma, 4 carcinomas and 3 metastases. The patient population was divided into two groups. Group 1 (n = 7) consisted of benign adrenal lesions. Group 2 consisted of malignant adrenal tumors. Lesion measurements were performed on the basis of the results of US, CT and/or MR images. In Group 1, no FDG uptake was observed in adrenal masses. Conversely, in Group 2 adrenal lesions showed abnormally increased FDG uptake, suggesting high glucose tumor metabolism. No significant difference in lesion size was observed between Groups 1 and 2 (5.6 +/- 4.0 vs 6.3 +/- 3.0 cm). Furthermore, in 6 patients of Group 2, total body PET images showed abnormal FDG uptake in extra-adrenal locations, such as chest (n = 2) and abdominal (n = 5) lymph nodes, lungs (n = 6), liver (n = 5), pancreas (n = 1), bone (n = 1) and muscle (n = 1) tissues. In conclusion, the results of this study suggest that PET imaging with FDG can characterize adrenal masses. In particular, abnormally increased FDG uptake in adrenal malignancies allows to differentiate these abnormalities from benign lesions. Furthermore, total body imaging PET can identify extra-adrenal tumor sites in patients with malignant tumor

    Copper-Catalyzed Decarboxylative C—N Cross-Coupling for N-Arylation

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    A novel approach for N-arylation utilizing aryl carboxylic acids as stable, inexpensive and widely available arylating reagents was developed. Employing a simple copper(II)-phenanthroline catalyst system, several benzoic acids bearing suitable ortho-substitutions undergo decarboxylative C—N cross-coupling effectively with various N-nucleophiles

    Evolution of a New Class of VEGFR‑2 Inhibitors from Scaffold Morphing and Redesign

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    Anti-VEGF therapy is a clinically validated treatment for age-related macular degeneration (AMD). We have recently reported the discovery of oral VEGFR-2 inhibitors that are selectively distributed to the ocular tissues. Herein we report a further development of those compounds and in particular the validation of the hypothesis that aminoheterocycles such as aminoisoxazoles and aminopyrazoles could also function as effective “hinge” binding moieties leading to a new class of KDR (kinase insert domain containing receptor) inhibitors
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