3 documents found, page 1 of 1
A selective p53 activator and anticancer agent to improve colorectal cancer the...
Ramos, H; Soares, MIL; Silva, J; Raimundo, L; Calheiros, J; Gomes, C; Reis, F; Monteiro, FA; Nunes, C; Reis, S; Bosco, B; Piazza, S; Domingues, LImpairment of the p53 pathway is a critical event in cancer. Therefore, reestablishing p53 activity has become one of the most appealing anticancer therapeutic strategies. Here, we disclose the p53-activating anticancer drug (3S)-6,7-bis(hydroxymethyl)-5-methyl-3-phenyl-1H,3H-pyrrolo[1,2-c]thiazole (MANIO). MANIO demonstrates a notable selectivity to the p53 pathway, activating wild-type (WT)p53 and restoring W...
SLMP53-2 restores wild-type-like function to mutant p53 through hsp70: Promisin...
Gomes, S; Bosco, B; Loureiro, JB; Ramos, H; Raimundo, L; Soares, J; Nazareth, N; Barcherini, V; Domingues, L; Oliveira, C; Bisio, A; Piazza, SHalf of human cancers harbor TP53 mutations that render p53 inactive as a tumor suppressor. In these cancers, reactivation of mutant p53 (mutp53) through restoration of wild-type-like function constitutes a valuable anticancer therapeutic strategy. In order to search for mutp53 reactivators, a small library of tryptophanol-derived oxazoloisoindolinones was synthesized and the potential of these compounds as mut...
Enhanced cytotoxicity of prenylated chalcone against tumour cells via disruptio...
Leão, M; Soares, J; Gomes, S; Raimundo, L; Ramos, H; Bessa, C; Queiroz, G; Domingos, S; Pinto, M; Inga, A; Honorina Cidade; Lucilia SaraivaAim Chalcones are naturally occurring compounds with recognized anticancer activity. It was recently shown that the O-prenyl derivative (2) of 2-hydroxy-3,4,4,5,6-pentamethoxychalcone (1) had a remarkably increased cytotoxicity against human tumour cells compared to its precursor. With this study, we aimed to investigate the molecular mechanism underlying the improved tumour cytotoxicity of prenylchalcone 2. Ma...