Marc Le Borgne
University Lyon 1
France
Title: Indeno[1,2-b]indoles: a good scaffold for designing bioactive molecules
Biography
Biography: Marc Le Borgne
Abstract
Indeno[1,2-b]indoles represent an important class of synthetic compounds for exploring drug targets. The great interest of these structures in Drug Design is due to the use of various building blocks to get the elemental four ring structure. Depending on the synthetic route chosen, the medicinal chemists can also achieve a large number of pharmacomodulations. Therefore, this presentation aims (i) to present an overview on how to access this family of heterocyclic compounds and (ii) to discuss their various biological applications in oncology (e.g. protein kinases and phosphatases) and in chemoresistance (e.g. ABC transporters). New biological investigations will be also presented.
Exploration of protein kinase CK2 by a functionalized indeno[1,2-b]indole
The presentation will cover several scientific disciplines to highlight our drug discovery programme dedicated to indeno[1,2-b]indoles. For example, organic syntheses (classical chemical process, “greener” methods), structural optimizations, CE-assay, Autodisplay technology, crystallography, docking, SAR and 3D-QSAR studies, rational design, complexation studies of cyclodextrins, cytotoxicity studies and so on will be presented and discussed.
The audience could notice how a research project started, made progress and allowed to build a ChemBio partners' network to share knowledge and results. Furthermore the success will depend on how chemists interfere with biologists. Both must investigate in all areas at the interface of chemistry and biology