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

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Access 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.

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Structure–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

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Meriolins (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

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Meriolins, 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.

Cancer Res. 2007, 67, 8325-8334

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