Pharmaceuticals (2019)
Update date:2022-08-11
Topics:
da Cruz, Anne Cecília Nascimento
Brondani, Dalci José
de Santana, Temístocles I′Talo
da Silva, Lucas Oliveira
Borba, Elizabeth Fernanda da Oliveira
de Faria, Ant?nio Rodolfo
de Albuquerque, Julianna Ferreira Cavalcanti
Piessard, Sylvie
Ximenes, Rafael Matos
Baratte, Blandine
Bach, Stéphane
Ruchaud, Sandrine
Mendon?a Junior, Francisco Jaime Bezerra
Bazin, Marc-Antoine
Rabello, Marcelo Montenegro
Hernandes, Marcelo Zaldini
Marchand, Pascal
da Silva, Teresinha Gon?alves
Fourteen arylsemicarbazone derivatives were synthesized and evaluated in order to find agents with potential anticancer activity. Cytotoxic screening was performed against K562, HL-60, MOLT-4, HEp-2, NCI-H292, HT-29 and MCF-7 tumor cell lines. Compounds 3c and 4a were active against the tested cancer cell lines, being more cytotoxic for the HL-60 cell line with IC50 values of 13.08 μμM and 11.38 μμM, respectively. Regarding the protein kinase inhibition assay, 3c inhibited seven different kinases and 4a strongly inhibited the CK1δ/ε kinase. The studied kinases are involved in several cellular functions such as proliferation, migration, cell death and cell cycle progression. Additional analysis by flow cytometry revealed that 3c and 4a caused depolarization of the mitochondrial membrane, suggesting apoptosis mediated by the intrinsic pathway. Compound 3c induced arrest in G1 phase of the cell cycle on HL-60 cells, and in the annexin V assay approximately 50% of cells were in apoptosis at the highest concentration tested (26 μμM). Compound 4a inhibited cell cycle by accumulation of abnormal postmitotic cells at G1 phase and induced DNA fragmentation at the highest concentration (22 μμM).
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