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Novel 7-Chloro-(4-thioalkylquinoline) Derivatives: Synthesis and Antiproliferative Activity through Inducing Apoptosis and DNA/RNA Damage

A series of 78 synthetic 7-chloro-(4-thioalkylquinoline) derivatives were investigated for cytotoxic activity against eight human cancer as well as 4 non-tumor cell lines. The results showed, with some exceptions, that sulfanyl <b>5</b>-<b>40</b> and sulfinyl <b>41</...

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Main Authors: Joyce E. Gutiérrez (Author), Esteban Fernandez-Moreira (Author), Miguel A. Rodríguez (Author), Michael R. Mijares (Author), Juan Bautista De Sanctis (Author), Soňa Gurská (Author), Petr Džubák (Author), Marián Hajdůch (Author), Julia Bruno-Colmenarez (Author), Luis Rojas (Author), Denis Deffieux (Author), Laurent Pouységu (Author), Stéphane Quideau (Author), Jaime Charris (Author), Hegira Ramírez (Author)
Format: Book
Published: MDPI AG, 2022-10-01T00:00:00Z.
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Summary:A series of 78 synthetic 7-chloro-(4-thioalkylquinoline) derivatives were investigated for cytotoxic activity against eight human cancer as well as 4 non-tumor cell lines. The results showed, with some exceptions, that sulfanyl <b>5</b>-<b>40</b> and sulfinyl <b>41</b>-<b>62</b> derivatives exhibited lower cytotoxicity for cancer cell lines than those of well-described sulfonyl N-oxide derivatives <b>63</b>-<b>82</b>. As for compound <b>81</b>, the most pronounced selectivity (compared against BJ and MRC-5 cells) was observed for human cancer cells from HCT116 (human colorectal cancer with wild-type p53) and HCT116p53−/− (human colorectal cancer with deleted p53), as well as leukemia cell lines (CCRF-CEM, CEM-DNR, K562, and K562-TAX), lung (A549), and osteosarcoma cells (U2OS). A good selectivity was also detected for compounds <b>73</b> and <b>74</b> for leukemic and colorectal (with and without p53 deletion) cancer cells (compared to MRC-5). At higher concentrations (5 × IC<sub>50</sub>) against the CCRF-CEM cancer cell line, we observe the accumulation of the cells in the G0/G1 cell phase, inhibition of DNA and RNA synthesis, and induction of apoptosis. In addition, X-ray data for compound <b>15</b> is being reported. These results provide useful scientific data for the development of 4-thioalkylquinoline derivatives as a new class of anticancer candidates.
Item Description:10.3390/ph15101234
1424-8247

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