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Synthesis and Development of Indole Based 5-HT3 Receptor Antagonists as Anti-Emetic Drugs in Oncology: An Update

[ Vol. 28 , Issue. 42 ]

Author(s):

Johana L. Rivera-Fonseca, Nelly González-Rivas, M. V. Basavanag Unnamatla, Marco A. García-Eleno, Horacio Reyes, L. Germán López-Valdez, David Corona-Becerril and Erick Cuevas-Yañez*   Pages 8733 - 8754 ( 22 )

Abstract:


An important group of antiemetic drugs used in the treatment of nausea and vomiting after chemotherapy containing an indole moiety in their structures, working as 5- hydroxytryptamine type 3 serotonin receptor antagonist (5-HT3). This study focuses on compounds bearing an indole core that present a 5-HT3 receptor antagonist activity, which have been successfully used as antiemetic drugs for reducing chemotherapy adverse secondary effects during cancer treatment. Their synthesis, biological activities, and some outstanding characteristics are discussed, providing a general outlook towards the development of more efficient antiemetic drugs.

Keywords:

Antiemetic drugs, 5-HT3, indole, synthesis, ondansetron, ramosetron, dolasetron, granisetron, ricasetron, tropisetron.

Affiliation:

Centro Conjunto de Investigación en Química Sustentable UAEM-UNAM, Carretera Toluca-Atlacomulco Km. 14.5, Toluca, Estado de México 50200, Centro Conjunto de Investigación en Química Sustentable UAEM-UNAM, Carretera Toluca-Atlacomulco Km. 14.5, Toluca, Estado de México 50200, Centro Conjunto de Investigación en Química Sustentable UAEM-UNAM, Carretera Toluca-Atlacomulco Km. 14.5, Toluca, Estado de México 50200, Centro Conjunto de Investigación en Química Sustentable UAEM-UNAM, Carretera Toluca-Atlacomulco Km. 14.5, Toluca, Estado de México 50200, División de Ingeniería Química, Tecnológico de Estudios Superiores de Jocotitlán. Carretera Toluca-Atlacomulco km 44.8, Ejido de San Juan y San Agustin, Jocotitlán, Edo, Laboratorio de Productos Naturales, Área de Química, Departamento de Preparatoria Agrícola, Universidad Autónoma Chapingo, Apartado 74, Oficina de Correos Chapingo, Km 38.5 carretera México-Texcoco, Chapingo, México 56230, Centro Conjunto de Investigación en Química Sustentable UAEM-UNAM, Carretera Toluca-Atlacomulco Km. 14.5, Toluca, Estado de México 50200, Centro Conjunto de Investigación en Química Sustentable UAEM-UNAM, Carretera Toluca-Atlacomulco Km. 14.5, Toluca, Estado de México 50200



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