Design and Synthesis of 2-Heterocyclyl-3-arylthio-1H-indoles as Potent Tubulin Polymerization and Cell Growth Inhibitors with Improved Metabolic Stability

Author:

La Regina Giuseppe1,Bai Ruoli2,Rensen Willeke3,Coluccia Antonio1,Piscitelli Francesco1,Gatti Valerio1,Bolognesi Alessio3,Lavecchia Antonio4,Granata Ilaria5,Porta Amalia5,Maresca Bruno5,Soriani Alessandra6,Iannitto Maria Luisa6,Mariani Marisa7,Santoni Angela36,Brancale Andrea8,Ferlini Cristiano7,Dondio Giulio9,Varasi Mario10,Mercurio Ciro11,Hamel Ernest2,Lavia Patrizia3,Novellino Ettore4,Silvestri Romano1

Affiliation:

1. Istituto Pasteur—Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Piazzale Aldo Moro 5, I-00185 Roma, Italy

2. Screening Technologies Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute at Frederick, National Institutes of Health, Frederick, Maryland 21702, United States

3. CNR, National Research Council, Institute of Molecular Biology and Pathology, Sapienza Università di Roma, Via degli Apuli 4, I-00185 Roma, Italy

4. Dipartimento di Chimica Farmaceutica e Tossicologica, Università di Napoli Federico II, Via Domenico Montesano 49, I-80131, Napoli, Italy

5. Dipartimento di Scienze Farmaceutiche, Sezione Biomedica, Università di Salerno, Via Ponte don Melillo, I-84084 Fisciano, Salerno, Italy

6. Dipartimento di Medicina Sperimentale e Patologia, Sapienza Università di Roma, Viale Regina Elena 324, I-00161 Roma, Italy

7. Danbury Hospital Research Institute, Tumor Reproductive Biology Research Laboratory, 131 West Street, Danbury, Connecticut 06810, United States

8. Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cardiff, CF10 3NB, U.K.

9. NiKem Research Srl, Via Zambeletti 25, 20021 Baranzate, Milano, Italy

10. European Institute of Oncology, Via Adamello 16, 20139 Milan, Italy

11. Genextra Group, DAC SRL, Via Adamello 16, 20139 Milan, Italy

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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