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Chimeric Drug Design With A Noncharged Carrier For Mitochondrial Delivery

Consuelo Ripoll, Pilar Herrero-Foncubierta, Virginia Puente-Muñoz, M. Carmen Gonzalez-Garcia, Delia Miguel, Sandra Resa, Jose M. Paredes, Maria J. Ruedas-Rama, Emilio Garcia-Fernandez, Mar Roldan, Susana Rocha, Herlinde De Keersmaecker, Johan Hofkens, Miguel Martin, Juan M. Cuerva, Angel Orte

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Recently, it was proposed that the thiophene ring is capable of promoting mitochondrial accumulation when linked to fluorescent markers. As a noncharged group, thiophene presents several advantages from a synthetic point of view, making it easier to incorporate such a side moiety into different molecules. Herein, we confirm the general applicability of the thiophene group as a mitochondrial carrier for drugs and fluorescent markers based on a new concept of nonprotonable, noncharged transporter. We implemented this concept in a medicinal chemistry application by developing an antitumor, metabolic chimeric drug based on the pyruvate dehydrogenase kinase (PDHK) inhibitor dichloroacetate (DCA). The promising features of the thiophene moiety as a noncharged carrier for targeting mitochondria may represent a starting point for the design of new metabolism-targeting drugs.