Day 1 :
Keynote Forum
Shaymaa E. Kassab
Associate Professor of Medicinal Chemistry
Keynote: Structure-based design and synthesis of conformationally constrained derivatives of methyl-piperidinopyrazole (MPP) with estrogen receptor (ER) antagonist activity
Time : 13:00-13:30
Biography:
Kassab is currently Associate Professor of Medicinal Chemistry at Faculty of Pharmacy-Damanhour University. In 2014, she joined a research group at the University of Maryland in Baltimore in the USA as a research fellow via a personal grant and patented a compound of therapeutic value against B call lymphoma. In 2016, she went back to USA as a research fellow at top universities there, Virginia Commonwealth and Texas A&M to learn and get trained on advanced research instruments and join research projects targeting neurological disorders. Her publications are in Q1-lead-international journals and specialized in Medicinal Chemistry and drug discovery. She focuses on designing novel compounds and developing others to be with minimized adverse effects and is selectively acting against the biological targets. She is a reviewer for Journal of Medicinal Chemistry, European Journal of Medicinal Chemistry and ACS Omega.
Abstract:
Nuclear Estrogen Receptors (ER) is cytoplasmic proteins; translocated to the nucleus to induce transcriptional signals after getting bound to the estrogen hormone. ER activation implicated in cancer cell proliferation of female reproductive organs. Thus, the discovery of ER antagonists is a reliable strategy to combat estrogen dependent breast cancer. Endometrial carcinoma is one of the complications encountered upon long-term therapy by Selective Estrogen Receptor Modulators (SERMs) like Tamoxifen (TMX) and Methyl Piperidino Pyrazole (MPP). Thus, the ER-full antagonist is a solution to improve the safety of this class of therapeutics during the treatment of breast cancer.
- Water Chemistry
Location: Barcelona, Spain
Session Introduction
Gabriele Micheletti
University of Bologna, Italy
Title: Synthesis and biological evaluation of novel Apcin analogues as potential CDC20 inhibitors
Biography:
Gabriele Micheletti is currently assistant in the Department of Industrial Chemistry at the University of Bologna. His field of specialization is organic chemistry and he has completed his studies in Industrial Chemistry in 2006, at the Faculty of Industrial Chemistry University of Bologna, Italy. In the 2011 he has pursued his PhD in Chemical Sciences at the same University. His fields of expertise are synthesis of novel organic compounds, organophosphorus chemistry, studies on mechanisms of organic chemistry reactions especially through detection of labile reaction intermediates by NMR spectroscopy (heteronuclear, dynamic variable temperature). Recent interest is in synthesis of new organic compounds of possible interest in biological field. He has more than 60 research publications in peer reviewed international journals
Abstract:
The research of compounds able to inhibit the interaction between APC/C and CDC20 has strongly emerged gaining a great deal of interest in recent years as useful tool for the design of CDC20 inhibitors, providing a therapeutic window in multiple human malignancies. Recently it has been discovered a new molecule called Apcin, which binds to CDC20, inhibiting the anaphase promoting complex into cells afflicted by AML (acute myeloid leukemia). In this context we planned the synthesis of a series of Apcin analogues (Figure 1), characterized by an amino aza-heterocycle moiety (in blue), bounded to a trichloroethyl group (in green) in turn functionalized with a pletora of group (in red) inserted through nucleophilic substitution to the precursor. Preliminary biological tests were carried out on the compounds obtained towards a panel of solid and hematological cancer cell lines.
Sepideh Madadkhani
Institute for Advanced Studies in Basic Sciences, Iran
Title: Electrocatalyst for water oxidation: Iron/Nickel/Zinc mixed oxide
Biography:
Sepideh Madadkhani is currently postdoctoral researcher in Institute for Advanced Studies in Basic Sciences (IASBS), Zanjan, Iran. She has a background in Inorganic Chemistry and focuses on Water Splitting. She is enthusiastic about transition metal compounds as electrocatalysts for sustainable energy conversion and storage applications. She is interested in developing operando experiments. Due to her years of research in the field of water oxidation, she was chosen as the best research student during her Ph.D. in her country
Abstract:
Statement of the Problem: Switching from fossil fuels to renewable energies is an inevitable task that should be performed in the near future to provide clean and sustainable energies for human beings. Water splitting toward hydrogen production is a promising approach to store such energies. In this regard, there are some bottlenecks for water splitting systems. Among different solutions, electrocatalytic water oxidation process is considered to be a breakthrough in water- splitting technology. Among the metal oxides, Ni/ Fe (oxy)hydroxide, which can be synthesized with different morphologies, stoichiometries and crystallinities, are able to catalyze the water-oxidation reaction in alkaline electrolyte solutions. Additionally, some research groups previously reported that Ni/Fe (oxy)hydroxides have the lowest overpotential toward water oxidation under the alkaline conditions. The purpose of this study is to describe a new procedure to synthesize an efficient Fe/Ni/Zn-based water-oxidizing catalyst by the thermal decomposition of a trimetallic organometallic compound. Characterization Methods: The catalyst were studied using scanning electron microscopy, transmission electron microscopy, electrochemical methods, X-ray diffraction, X-ray absorption spectroscopy, and X-ray photoelectron spectroscopy. Findings: In addition to Ni and Fe as important ions for water oxidation, the present organometallic compound includes Zn ion as an amphoteric ion which can be removed in the presence of KOH solution to obtain more active sites on the surface of the catalyst and thus a self-improvement is observed during reaction. On the basis of the obtained results, a structure similar to (Ni, Zn)Fe2O4 is proposed. The obtained nanosized oxide on FTO at pH=13 showed a current density of 12 mA/cm2 at 1.2 V. Long-time amperometry also indicated an increase in the current density. Continued CVs showed that the water-oxidizing activity of the compound increased during the cyclic voltammetry process. Since Zn ions are amphoteric, they can be soluble in KOH solution and results in a self-improvement for the catalyst. Removing the Zn ions from the NiFeZnOx structure may be a promising method to increase the catalytic activity of the present oxide. Conclusion & Significance: Introducing a new procedure to synthesize an efficient Fe/Ni/Zn-based water-oxidizing catalyst by the thermal decomposition of a trimetallic organometallic compound. The catalyst showed a good long-term stability and performance. The composition of the compound was characterized by some common methods and found to be an efficient wateroxidizing catalyst.