Dear all,
on behalf of the Organising Committee and the COST Action CA18122 EURO-CHOLANGIO-NET we welcome you to the training school on “drug discovery and chemoresistance in cholangiocarcinoma” to be held 1-2 June 2023, in Porto Rio Hotel, Patras, Greece.
Looking forward to meeting you all in Patras,
Kind regards
Prof. Constantinos M. Athanassopoulos
The main objective of this course is to optimize knowledge regarding drug discovery and testing in cholangiocarcinoma.
Topics that will be covered during the training school include:
Day I, Session I: Cholangiocarcinoma: general aspects, heterogenicity, molecular aspects; in vitro and in vivo models; development of biologically useful novel chemical entities (NCEs); preclinical stages; clinical trials; generation of small molecule NCEs; chemical synthesis; convergent and linear routes; combinatorial libraries; atom economy; sustainability; scaling; semi-synthesis; coupling of synthetic units with natural products; conjugation with biomolecules; coupling with basic and acidic residues.
Day I, Session II: Evaluation and prediction of biological properties; high-throughput screening (HTS) of chemical libraries; rational design of drugs; in-silico evaluation of potency and ADME(Tox) properties of drug candidates; Euclidean and non-Euclidean metrics; selection rules; molecular modelling: docking, atomistic models, QSAR; drug resistance; mechanisms of multidrug resistance phenotype; analysing drug transport dynamics; Darwinian models; protection and publication of results about NCEs; writing patents: general structures, state of the art, description, examples, claims, inventors; phases (and costs) of patent filing.
Day II: Developments in NCEs against cholangiocarcinoma and case studies
