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- Title
Novel 7-Chloro-(4-thioalkylquinoline) Derivatives: Synthesis and Antiproliferative Activity through Inducing Apoptosis and DNA/RNA Damage.
- Authors
Gutiérrez, Joyce E.; Fernandez-Moreira, Esteban; Rodríguez, Miguel A.; Mijares, Michael R.; De Sanctis, Juan Bautista; Gurská, Soňa; Džubák, Petr; Hajdůch, Marián; Bruno-Colmenarez, Julia; Rojas, Luis; Deffieux, Denis; Pouységu, Laurent; Quideau, Stéphane; Charris, Jaime; Ramírez, Hegira
- Abstract
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 5–40 and sulfinyl 41–62 derivatives exhibited lower cytotoxicity for cancer cell lines than those of well-described sulfonyl N-oxide derivatives 63–82. As for compound 81, 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 73 and 74 for leukemic and colorectal (with and without p53 deletion) cancer cells (compared to MRC-5). At higher concentrations (5 × IC50) 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 15 is being reported. These results provide useful scientific data for the development of 4-thioalkylquinoline derivatives as a new class of anticancer candidates.
- Subjects
DNA synthesis; DNA; RNA; CANCER cells; CELL lines; SULFONYL compounds
- Publication
Pharmaceuticals (14248247), 2022, Vol 15, Issue 10, p1234
- ISSN
1424-8247
- Publication type
Article
- DOI
10.3390/ph15101234