SMITh
For many years, the SMITh team has been devoted to the development of drug candidates and pharmacological tools, mainly in the field of cancer. The drug candidates are either small molecules (ALDH inhibitors) or antibody drug conjugates (ADC) using innovative technologies developped by SMITh team and partners. The pharmacological tools concern RNA binders (homocarbonyltopsentin - PK4C9 with application in spinal muscular atrophy), kinase inhibitors (finisterin and meriolin series as potent anticancer drugs) and transglutaminase inhibitors (BJJF078).
Publications Find the most recent scientific contributions
Room temperature and transition-metal-free intramolecular α-arylation of ketones: a mild access to tetracyclic indoles and 7-aza indoles
Adouama, Chérif; Buden, Maria Eugenia; Guerra, Walter Damian; Puiatti, Marcelo; Joseph, Benoît; Barolo, Sylvia M; Rossi, Roberto Arturo; Médebielle, Maurice
Org. Lett. 2019, 21, 320-324
Read the whole publicationAccess to cyclic gem-difluoroacyl scaffolds via electrochemical and visible light photocatalytic radical tandem cyclization of heteroaryl chlorodifluoromethyl ketones
C. Adouama, R. Keyrouz, G. Pilet, C. Monnereau, D. Gueyrard, T. Noel, M. Médebielle*
Chem. Commun., 2017, 53, 5653-5656.
Read the whole publicationStructure–Activity Relationship of S-Trityl-l-Cysteine Analogues as Inhibitors of the Human Mitotic Kinesin Eg5
DeBonis, S.; Skoufias, D.A.; Indorato, R.-L.; Liger, F.; Marquet, B.; Laggner, C.; Joseph, B.; Kozielski, F.
J. Med. Chem. 2008, 51, 1115-1125
Read the whole publicationMeriolins (3-(Pyrimidin-4-yl)-7-azaindoles): Synthesis, Kinase Inhibitory Activity, Cellular Effects, and Structure of a CDK2/CyclinA/Meriolin Complex
Echalier, A.; Bettayeb, K.; Ferandin, Y.; Lozach, O.; Clement, M.; Valette, A.; Liger, F.;Marquet, B.; Morris, J.C.; Endicott, J.A.; Joseph, B.; Meijer, L.
J. Med. Chem. 2008, 51, 737-751
Read the whole publicationMeriolins, a New Class of CellDeath-Inducing Kinase Inhibitors with Enhanced Selectivity for Cyclin-Dependent Kinases
Bettayeb, K.; Tirado, O.M.; Marionneau-Lambot, S.; Ferandin, Y.; Lozach, O.; Morris, J.C.;Mateo-Lozano, S.; Drueckes, P.; Schaechtele, C.; Kubbutat, M.H.G.; Liger, F.; Marquet, B.;Joseph, B.; Echalier, A.; Endicott, J.A.; Notario, V.; Meijer, L.