Gutiérrez, Joyce E.Fernández Moreira, EstebanRamírez, Hegira2025-10-212025-10-212022-10-08Gutiérrez, J.E.; Fernandez-Moreira, E.; Rodríguez, M.A.; Mijares, M.R.; De Sanctis, J.B.; Gurská, S.; Džubák, P.; Hajdůch, M.; Bruno-Colmenarez, J.; Rojas, L.; et al. Novel 7-Chloro-(4-thioalkylquinoline) Derivatives: Synthesis and Antiproliferative Activity through Inducing Apoptosis and DNA/RNA Damage. Pharmaceuticals 2022, 15, 1234. https://doi.org/10.3390/ph1510123410.3390/PH15101234https://hdl.handle.net/20.500.14352/125143A 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.engAttribution 4.0 Internationalhttp://creativecommons.org/licenses/by/4.0/journal article1424-8247https://doi.org/10.3390/ph15101234https://www.mdpi.com/1424-8247/15/10/1234open access615.01/.03Antiproliferative activityCell cycleDNA/RNA damageSynthesis of 4-thioalkylquinolineSulfanyl-Sulfinyl-Sulfonyl groupsCiencias BiomédicasFarmacología (Medicina)32 Ciencias Médicas3209 Farmacología