RT Journal Article
T1 Chimeric Drug Design with a Noncharged Carrier for Mitochondrial Delivery
A1 Ripoll, Consuelo
A1 Herrero-Foncubierta, Pilar
A1 Puente-Muñoz, Virginia
A1 Gonzalez-Garcia, M. Carmen
A1 Miguel, Delia
A1 Resa, Sandra
A1 Paredes, Jose M.
A1 Ruedas-Rama, Maria J.
A1 Garcia-Fernandez, Emilio
A1 Roldan, Mar
A1 Rocha, Susana
A1 De Keersmaecker, Herlinde
A1 Hofkens, Johan
A1 Martin, Miguel
A1 Cuerva, Juan M.
A1 Orte, Angel
K1 Antitumor agents
K1 Fluorescence lifetime imaging
K1 Medicinal chemistry
K1 Metabolic drug
K1 Mitochondrial carrier
K1 Antineoplásicos
K1 Química farmacéutica
K1 Activación metabólica
K1 Tiofenos
K1 Mitocondrias
AB 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.
PB MDPI
YR 2021
FD 2021-02-12
LK http://hdl.handle.net/10668/3874
UL http://hdl.handle.net/10668/3874
LA en
NO Ripoll C, Herrero-Foncubierta P, Puente-Muñoz V, Gonzalez-Garcia MC, Miguel D, Resa S, et al. Chimeric Drug Design with a Noncharged Carrier for Mitochondrial Delivery. Pharmaceutics. 2021 Feb 12;13(2):254
DS RISalud
RD Apr 11, 2025