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Anticancer properties of indole derivatives as IsoCombretastatin A-4 analogues.
Pecnard, Shannon; Hamze, Abdallah; Bignon, Jérome; Prost, Bastien; Deroussent, Alain; Gallego-Yerga, Laura; Peláez, Rafael; Paik, Ji Yeon; Diederich, Marc; Alami, Mouad; Provot, Olivier.
Affiliation
  • Pecnard S; Université Paris-Saclay, CNRS, BioCIS, 92290, Châtenay-Malabry, France.
  • Hamze A; Université Paris-Saclay, CNRS, BioCIS, 92290, Châtenay-Malabry, France. Electronic address: abdallah.hamze@universite-paris-saclay.fr.
  • Bignon J; Institut de Chimie des Substances Naturelles, UPR 2301, CNRS Avenue de La Terrasse, F-91198, Gif sur Yvette, France.
  • Prost B; Service D'Analyse des Médicaments et Métabolites, IPSIT, Univ. Paris-Sud, UMS 3679 CNRS, US 31 INSERM, Université Paris-Saclay, 92290, Châtenay Malabry, France.
  • Deroussent A; Metabolic and Systemic Aspects of Oncogenesis (METSY), UMR 9018, CNRS, Institut Gustave Roussy, Université Paris-Saclay, 94805, Villejuif, France.
  • Gallego-Yerga L; Laboratorio de Química Orgánica y Farmacéutica, Departamento de Ciencias Farmacéuticas, Facultad de Farmacia, Universidad de Salamanca, Salamanca, Spain.
  • Peláez R; Laboratorio de Química Orgánica y Farmacéutica, Departamento de Ciencias Farmacéuticas, Facultad de Farmacia, Universidad de Salamanca, Salamanca, Spain.
  • Paik JY; Department of Pharmacy, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 08626, South Korea.
  • Diederich M; Department of Pharmacy, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 08626, South Korea.
  • Alami M; Université Paris-Saclay, CNRS, BioCIS, 92290, Châtenay-Malabry, France. Electronic address: mouad.alami@universite-paris-saclay.fr.
  • Provot O; Université Paris-Saclay, CNRS, BioCIS, 92290, Châtenay-Malabry, France. Electronic address: olivier.provot@universite-paris-saclay.fr.
Eur J Med Chem ; 223: 113656, 2021 Nov 05.
Article in En | MEDLINE | ID: mdl-34171660
ABSTRACT
In this study, a variety of original ligands related to Combretastatin A-4 and isoCombretastatin A-4, able to inhibit the tubulin polymerization into microtubules, was designed, synthesized, and evaluated. Our lead compound 15d having a quinazoline as A-ring and a 2-substituted indole as B-ring separated by a N-methyl linker displayed a remarkable sub-nanomolar level of cytotoxicity (IC50 < 1 nM) against 9 human cancer cell lines.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Stilbenes / Tubulin Modulators / Indoles / Antineoplastic Agents Limits: Animals / Humans Language: En Journal: Eur J Med Chem Year: 2021 Document type: Article Affiliation country:
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Stilbenes / Tubulin Modulators / Indoles / Antineoplastic Agents Limits: Animals / Humans Language: En Journal: Eur J Med Chem Year: 2021 Document type: Article Affiliation country: