%0 Journal Article
%A Ripoll, Consuelo
%A Herrero-Foncubierta, Pilar
%A Puente-Muñoz, Virginia
%A Gonzalez-Garcia, M Carmen
%A Miguel, Delia
%A Resa, Sandra
%A Paredes, Jose M
%A Ruedas-Rama, Maria J
%A Garcia-Fernandez, Emilio
%A Roldan, Mar
%A Rocha, Susana
%A De Keersmaecker, Herlinde
%A Hofkens, Johan
%A Martin, Miguel
%A Cuerva, Juan M
%A Orte, Angel
%T Chimeric Drug Design with a Noncharged Carrier for Mitochondrial Delivery.
%D 2021
%@ 1999-4923
%U https://hdl.handle.net/10668/28415
%X 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.
%K antitumor agents
%K fluorescence lifetime imaging
%K medicinal chemistry
%K metabolic drug
%K mitochondrial carrier
%~