Institut de Chimie Organique et Analytique (ICOA)
Chimie hétérocyclique à visée thérapeutique
Tél. : +33 (0)2 38 49 48 53
- Loiret (45)
- Centre – France
Research in the Routier group is directed toward molecular innovation in medical therapy, with the ultimate goal being the development of drug candidates for the diagnosis or treatment of diverse pathologies. For over 10 years this group has directed their research toward various molecular targets involved in the areas of Alzheimer’s disease, Parkinson’s disease, multiple sclerosis, diabetes, and above all, cancer.
The group is made up of three permanent researchers (1 full professor, 1 assistant professor and 1 CNRS researcher) as well as collaborators at all levels (postdoctoral fellows, PhD students, technicians, and undergraduate students). Our goal is to fully explore the known chemical space and expand reactivity through the functionalization of rare heterocycles which can be further transformed into potential drug candidates. Our innovative synthetic methods, original chemical scaffolds and activity with leading edge molecular targets are regularly published as patents and articles in respected academic journals.
The major expertise in our laboratory, recognized on a national and international level, is the use of transition metal catalyzed reactions using microwave irradiation, the formation and reactivity of the acylium ion, the enantioselective synthesis of spirocyclique compounds, as well as thermodynamic and photochemical cyclization reactions. We are also involved in the field of radiolabeling with the synthesis of synthetic precursors necessary for the incorporation of 18F and 11C.
Our group is interested in discovering new technologies to overcome problems frequently encountered in synthetic organic chemistry through the use of microwave and UV irradiation, flow chemistry, and product purification using up-to-date flash chromatography techniques. This in turn will positively influence the time and effort spent in in chemical synthesis and purification steps, as well as decrease solvent use and waste by-products. Methodology developed in this area is part of an environmentally responsible approach to organic chemistry.
Taken together, our know-how has led to the synthesis of numerous active compounds which selectively target enzymes (kinases, topoisomerases), G protein-coupled receptors (ROR, PPAR), integrins (VLA4), and ion channels (nAchR, KCNQ2, SK). The group has collectively published 68articles and has 5 national and international patents, the majority of which are the result of translational research projects. Furthermore, the group is one of the partners of the Labex IRON (Innovation Radiopharmaceuticals in Oncology and Neuropathologies) and SYNORG (Organic Synthesis and Scaffold developments).
Role in the network
We offer to projects our strong expertise in design original and efficient compounds via a molecular modeling studies and synthesis of library. Actually, in collaboration with C. Vandier’s team at Tours, research funded by the Ligue Contre le Cancer, we use our expertise to undertake the rational synthesis/characterization of novel SK3 channel inhibitors. For instance, a few products are already shown an inhibition of SK3 channel with anti-metastatic properties as the imidazopyrimidine NS-8593. Using this modulator as reference, we purpose to develop a pharmacological model M1 in the respect of the major structural requirement, as including a fraction guanidine function, related to enhance the regulation of this channel. They will next offer their expertise to design other selective drugs targeting for example ORAI target.
Involvement in tasks 3
Co-coordinator of task 3- Sylvain Routier : Discovery of SK3 and SOC modulators