Small Molecular Antagonists
Prof. Raid Abdel-Jalil
Sultan Qaboos University
Prof. Raphael Stoll
Faculty of Chemistry and Biochemistry
Abdel-Jalil, R. J. is Associate Professor in organic chemistry at the Department of Chemistry at Sultan Qaboos University. He was a postdoctoral research fellow in Crump Institute for Molecular Imaging at UCLA. Abdel-Jalil, R.J. earned his doctoral degree in Organic Chemistry at Tuebingen University, Germany under the auspices of German Academic Exchange Service (DAAD) Fellowship. He obtained a Master of Science degree and a Bachelor of Chemistry degree from the University of Jordan, Jordan. Abdel-Jalil is the authored/co-authored of over 40-refereed scientific articles as of May 2016. His research interests include development of new methods in organic synthesis, synthesis of biological active compounds and chemical modification of stationary phases. Abdel-Jalil has developed several new methods in chiral and achiral synthesis of heterocyclic systems.
Project Summary & Research Plan
Protein-ligand binding is one of the cornerstones in medicinal chemistry to develop lead compounds for many diseases, such as cancer for instance. Elucidating the mechanism(s) of protein-ligand binding is an essential step towards optimising drug formulae and maximising drug potency and efficacy. We envisage to synthesise drug-like molecules for small GTPases and to investigate the nature of the protein-ligand binding sites by biomolecular NMR spectroscopy.
This VIP project consists of two parts:
- We plan to synthesise and structurally elucidate new compounds and their corresponding intermediates.
- We aim to determine the three-dimensional structures and to analyse the dynamics of these biomolecules as well as their interaction with these newly synthesised compounds in solution at near-physiological conditions using multidimensional NMR spectroscopy.
Activities in 2016
Prof. Abdel-Jalil visited RUB in 2016 in July, August, and in January 2017. During the summer term of 2016 he offered a lecture series on applied spectroscopy. Furthermore, he discussed research ideas and projectes with PhD students of the Faculty of Chemistry and Biochemistry. In December 2016, Prof. Abdel-Jalil and Raphael Stoll participated at the PHARMAMED-2016 conference in Dubai, UAE, in order to present their research results.
Activities in 2017
Prof. Abdel-Jalil visited RUB in January, July and August. During the summer term of 2017 he offered a lecture series on the disconnection approach in organic chemistry and he discussed again research ideas and projects with PhD students of the Faculty of Chemistry and Biochemistry.
In addition, we could secure travel funds from the RUB Research SchoolPlus that will enable a PhD student from Bochum to visit SQU in Oman for a period of four weeks in 2018. During this stay, the PhD will join Prof. Abdel-Jalil’s laboratory as a guest scientist.
- Al-Harthy T, Zoghaib WM, Pflüger M, Schöpel M, Önder K, Reitsammer M, Hundsberger H, Stoll R, Abdel-Jalil R. (2016) Design, Synthesis, and Cytotoxicity of 5-Fluoro-2-methyl-6-(4-aryl-piperazin-1-yl) Benzoxazoles. Molecules 21(10). pii: E1290..
- Schöpel M., Potheraveedu V.N., Al-Harthy T., Abdel-Jalil R., Heumann R., Stoll R. (2017) The small GTPases Ras and Rheb studied by multidimensional NMR spectroscopy: Structure and Function. Biological Chemistry, 398:577-588.
- Arnolds O., Zhong X., Yip K.T., Schöpel M., Kohl B., Pütz S., Abdel-Jalil R., Stoll R. (2017) NMR-based drug development and improvement against malignant melanoma - implications for the MIA protein family. Current Medicinal Chemistry, 24:1788-1796.
- Al-Harthy T, Zoghaib WM, Stoll R, Abdel-Jalil R. (2018) Design, synthesis, and antimicrobial evaluation of novel 2-arylbenzothiazole analogs bearing fluorine and piperazine moieties. Monatshefte Chemie, DOI 10.1007/s00706-017-2088-4.