Genotoxicity and Anticancer Effects of the Aminothiophene Derivatives SB-44, SB- 83, and SB-200 in Cancer Cells

Author(s):

Eduardo Davi Lima da Silva, Flaviana Alves dos Santos, Júlia Teixeira de Oliveira, Fabio Vieira dos Santos, Francisco Jaime Bezerra Mendonça Junior, Maria do Carmo Alves de Lima, Maira Galdino da Rocha Pitta, Moacyr Barreto de Jesus de Melo Rego and Michelly Cristiny Pereira*   Pages 1447 - 1456 ( 10 )

Abstract:

<p>Introduction: Thiophene derivatives have been widely studied as promising options for the treatment of solid tumors. Previous studies have shown that thiophene derivatives have antileishmanial activity and cytotoxic activity against breast, colon, and ovarian cancer cells. </p><p> Methods: In our study, we evaluated the anticancer activities of three aminothiophene derivatives: SB-44, SB-83, and SB-200, in prostate and cervical adenocarcinoma cells. Several in vitro methods were performed, including cytotoxicity, clonogenic migration, mutagenic, and cleaved Poly (ADP-ribose) polymerase (PARP) assays and annexin V staining. </p><p> Results: Significant cytotoxicity was observed in cell lines with IC50 values less than 35 μM (15.38-34.04 μM). All aminothiophene derivatives significantly reduced clone formation but had no effect on cell motility. SB-83 and SB-44 induced a significant increase in the percentage of cells in the sub-G1 phase, while SB-200 derivatives significantly decreased the percentage of S/G2/M as well as induced apoptosis, with an increase of cleaved PARP. SBs compounds also showed significant mutagenic potential. Beyond that, in silico analyses revealed that all three thiophene derivatives fulfilled the criteria for oral druggability, which underscores the potential of using them in anticancer therapies. </p><p> Conclusion: Our findings show that the thiophene nucleus may be used to treat solid tumors, including prostate cancer and cervical adenocarcinoma.</p>

Keywords:

Anticancer effect, prostate cancer, thiophene, genotoxicity, proliferation, apoptosis.

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