Design, synthesis and biological evaluation of novel cyano-cinnamate derivatives as mitochondrial pyruvate carrier inhibitors.
Bioorg Med Chem Lett
; 112: 129923, 2024 Aug 10.
Article
en En
| MEDLINE
| ID: mdl-39134097
ABSTRACT
Mitochondrial pyruvate carrier (MPC) inhibitors promote the development of hair follicle stem cells without affecting normal cells, which is promising for the treatment of hair loss. Herein, a series of cyano-cinnamate derivatives of UK-5099 were designed and synthesized. All these new compounds have been tested for their ability to promote cellular lactate production in vitro. Compound 4i (LA content0.322 µmol/106cell) showed better cellular lactate production activity than UK-5099 (LA content0.185 µmol/106cell). Further compound 4i was also tested on shaved mice by topical treatment and promoted obvious hair growth on mice.
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Bases de datos:
MEDLINE
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En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2024
Tipo del documento:
Article
País de afiliación:
China