Synthetic thiophenes induce chromosomal damage and trigger apoptosis in human cancer cell lines

Franco, Filipe Nogueira; Oliveira, Jorge de; Tecchio, Kimberly Brito; Santos, Flaviana Alves dos; Rego, MJ; Mendonça-Junior, Francisco Jaime Bezerra; Pitta, M. G. R.; Pereira, Michelly Cristiny; Ribeiro, Rosy Iara Maciel Azambuja; Santos, Vanessa J. S. V.; Santos, Fábio V.

doi:10.1016/j.ejmcr.2022.100033

Cited by 2 publications

(1 citation statement)

References 25 publications

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“…Furthermore, and according to the literature, thiophene-based compounds have applications ranging from anti-cancer chemotherapy to the treatment of a variety of other diseases [27,28]. Several human tumor cell lines, including cervical cancer, gastric cancer, colorectal cancer, oesophageal cancer, lung cancer, hepatocellular carcinoma, oral cancer, osteosarcoma, prostate cancer, ovarian cancer, and breast carcinoma, have shown inhibitory activity in vitro and in vivo [29][30][31][32][33][34][35][36]. The chloroacetamides possess key structural features, including an easy replacement of chlorine atoms, which make them highly attractive synthetic platforms for synthesizing diverse heterocyclic systems.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of some new thiophene-based compounds and evaluations of their cytotoxic activities

Mehdhar¹,

Alzahrani²,

Abdel‐Galil³

et al. 2022

Bull. Chem. Soc. Eth.

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ABSTRACT. A series of new thiophene derivatives was prepared through nucleophilic substitution reactions of the precursor N-(4-substituted-phenyl)-5-(2-chloroacetamido)-4-cyano-3-methylthiophene-2-‎carboxamides 4a and 4b with different sulfur and/or nitrogen nucleophilic reagents (namely; mercaptoacetic acid, 2-mercaptobenzothiazole, 5-(phenylamino)-1,3,4-thiadiazole-2-thiol, 2-mercapto-4,6-dimethylnicotinonitrile, 3-arylazo-4-mercapto-4-(phenylamino)-but-3-en-one derivatives, ammonium thiocyanate, piperidine and/or morpholine). The structures of the prepared thiophene compounds were characterized by spectral analysis. Their cytotoxicity was evaluated against two human cancer cell lines (HepG2 and MCF-7) and indicated promising results. Pretreatment of HepG2 cells with the tested compound 4b sensitized the cells to the cytotoxicity of sorafenib, leading to a significant decrease in the IC50 from 3.9 to 0.5 µM. KEY WORDS: N-(Thienyl)-2-chloroacetamide, Bis-thiophene, Thieno[2,3-d]pyrimidine, Ammonium thiocyanate, Cytotoxicity Bull. Chem. Soc. Ethiop. 2023, 37(2), 373-389. DOI: https://dx.doi.org/10.4314/bcse.v37i2.10

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Section: Introductionmentioning

confidence: 99%

Synthesis of some new thiophene-based compounds and evaluations of their cytotoxic activities

Mehdhar¹,

Alzahrani²,

Abdel‐Galil³

et al. 2022

Bull. Chem. Soc. Eth.

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A decade's overview of 2‐aminothiophenes and their fused analogs as promising anticancer agents

Darwish,

El‐Sherief,

Abdel‐Aziz

et al. 2024

Archiv der Pharmazie

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Over the past decades, cancer has been a challenging domain for medicinal chemists as it is an international health concern. In association, small molecules such as 2‐aminothiophenes and their derivatives showed significant antitumor activity through variable modes of action. Therefore, this article aims to review the advances regarding these core scaffolds over the past 10 years, where 2‐aminothiophenes and their fused analogs are classified and discussed according to their biological activity and mode of action, in the interest of boosting new design pathways for medicinal chemists to develop targeted antitumor candidates.

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Synthetic thiophenes induce chromosomal damage and trigger apoptosis in human cancer cell lines

Cited by 2 publications

References 25 publications

Synthesis of some new thiophene-based compounds and evaluations of their cytotoxic activities

Synthesis of some new thiophene-based compounds and evaluations of their cytotoxic activities

A decade's overview of 2‐aminothiophenes and their fused analogs as promising anticancer agents

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