A5079713482- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Catalytic Cross-Coupling Reactions
- Catalytic C–H Functionalization Methods
- Organoboron and organosilicon chemistry
- Cholangiocarcinoma and Gallbladder Cancer Studies
- Blood properties and coagulation
- Cell death mechanisms and regulation
- Lung Cancer Treatments and Mutations
- Lymphoma Diagnosis and Treatment
- Erythrocyte Function and Pathophysiology
- Cancer Genomics and Diagnostics
- Chemical Synthesis and Analysis
- Vascular Tumors and Angiosarcomas
- Sarcoma Diagnosis and Treatment
- Healthcare cost, quality, practices
- Epigenetics and DNA Methylation
- Liver physiology and pathology
- Chemical synthesis and alkaloids
- Viral-associated cancers and disorders
- Crystallography and molecular interactions
- Sulfur-Based Synthesis Techniques
- Melanoma and MAPK Pathways
- Digital Imaging for Blood Diseases
- Metal complexes synthesis and properties
University of Bristol
2018-2024
Cardiff University
2017
University of Milan
2005-2016
European Institute of Oncology
2005-2012
University of Szeged
2012
Uppsala University
2012
The cobalt-catalyzed Suzuki biaryl cross-coupling of aryl chloride substrates with boron reagents, activated more commonly used bases, remained a significant unmet challenge in the race to replace platinum group metal catalysts Earth-abundant alternatives. We now show that this highly desirable process can be realized using alkoxide provided right counterion is employed, strict stoichiometric control base maintained respect reagent, and correct ester selected. Potassium tert-butoxide works...
Herein we report the metal-free diastereoselective frustrated Lewis pair (FLP)-catalyzed hydrogenation of aza-Morita–Baylis–Hillman (aza-MBH) adducts, accessing a diverse range stereodefined β-amino acid derivatives in excellent isolated yields (28 examples, 89% average yield, up to 90:10 d.r.). Furthermore, sequential organo-FLP catalysis has been developed. An initial organocatalyzed aza-MBH reaction followed by situ FLP formation and electron-deficient α,β-unsaturated carbonyl compounds...
Intrigued by recent reports on the surprisingly excellent activity of a range cobalt-, iron-, copper-, and nickel-based catalysts in Suzuki biaryl cross-coupling simple aryl boronic acids with halides, we undertook reexamination syntheses representative examples reported precatalysts their application to catalytic reaction. A PNP−Fe pincer complex proved be mixture starting materials; mono-Schiff base cobalt fact bis-ligated adduct monomeric copper(II) PNP–pincer di- or oligomeric copper(I)...
The rational design, synthesis and in vitro biological evaluation of dual action conjugates 11-13, containing a tumour targeting, integrin αvβ3/αvβ5 ligand portion pro-apoptotic SMAC mimetic (cyclo-RGD/SMAC conjugates) are reported. binding strength the two separate units is generally maintained by these conjugates. In particular, connection between (anchor points on each unit; nature, length stability linker) influences activity against its molecular targets (integrins for cyclo-RGD, IAP...
Edaravone is a neuroactive drug that currently used in the treatment of stroke patients and shows promise against range neurodegenerative processes including amyotrophic lateral sclerosis, Parkinson's disease Alzheimer's disease. We show iron-catalysed C-H functionalisation edaravone its derivatives can be exploited to generate small library 21 arylated edaravones, while results preliminary computational binding study these predicts they should all bind more strongly active site monoamine...
1058 Background: BRCA1 plays a central role repairing DNA double-strand breaks via homologous recombination (HR). The large majority of breast cancers in germinal mutation carriers express the triple-negative phenotype, unresponsive to currently available ER-targeted and HER2-based treatments. Even wild type (wt) TNBC, clinical behaviour can be similar with aggressive course, limited treatment options poor prognosis (“bracaness” tumors). Another important damage repair enzyme, MGMT, is...
14145 Background: Both MTA and GCB are active drugs in non-small cell lung cancer (NSCLC). Many molecular events induced by support the synergic interaction between two explain why sequence ? is more than MTA. Of major interest, induces expression of deoxycytidine kinase (dCK), rate-limiting enzyme activation, human equilibrative nucleoside transporter-1 (hENT1), key transporter for intracellular penetration GCB. Even if optimal well established, no information on best administration time...
14644 Background: A number of pharmacogenomic studies have been recently carried out to find a possible relationship between gene expression and treatment outcome in NSCLC; however, our knowledge, no data are available on the influence tumor histology stage profile. The aim this study was characterization pattern genes involved gemcitabine cisplatin activity primary or metastatic adenocarcinoma squamous carcinoma NSCLC specimens. Methods: Excision repair cross-complementing 1 (ERCC1), human...