Biological Evaluation of Arylsemicarbazone Derivatives as Potential Anticancer Agents

Biological Evaluation of Arylsemicarbazone Derivatives as Potential Anticancer Agents

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 and were active against the tested cancer cell...

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Published in:Pharmaceuticals (Basel, Switzerland) Vol. 12; no. 4; p. 169
Main Authors: Nascimento da Cruz, Anne Cecília, Brondani, Dalci José, I Talo de Santana, Temístocles, Oliveira da Silva, Lucas, da Oliveira Borba, Elizabeth Fernanda, de Faria, Antônio Rodolfo, Ferreira Cavalcanti de Albuquerque, Julianna, Piessard, Sylvie, Matos Ximenes, Rafael, Baratte, Blandine, Bach, Stéphane, Ruchaud, Sandrine, Bezerra Mendonça Junior, Francisco Jaime, Bazin, Marc-Antoine, Montenegro Rabello, Marcelo, Hernandes, Marcelo Zaldini, Marchand, Pascal, Gonçalves da Silva, Teresinha
Format: Journal Article
Language:English
Published: Switzerland MDPI AG 17-11-2019
MDPI
Subjects:
anticancer activity
apoptosis
Cancer
Cancer therapies
Cell cycle
Cell division
Chemical Sciences
Chemotherapy
Cyclin-dependent kinases
Cytotoxicity
kinase inhibition
Kinases
Life Sciences
Medical research
Medicinal Chemistry
Proteins
semicarbazones
Signal transduction
semicarbazones
apoptosis
anticancer activity
kinase inhibition
cell cycle
cytotoxicity
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Summary: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 and were active against the tested cancer cell lines, being more cytotoxic for the HL-60 cell line with IC values of 13.08 μM and 11.38 μM, respectively. Regarding the protein kinase inhibition assay, inhibited seven different kinases and 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 and caused depolarization of the mitochondrial membrane, suggesting apoptosis mediated by the intrinsic pathway. Compound 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 μM). Compound inhibited cell cycle by accumulation of abnormal postmitotic cells at G1 phase and induced DNA fragmentation at the highest concentration (22 μM).
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ISSN:1424-8247
1424-8247
DOI:10.3390/ph12040169