Journal
PHARMACEUTICALS
Volume 15, Issue 10, Pages -Publisher
MDPI
DOI: 10.3390/ph15101234
Keywords
antiproliferative activity; cell cycle; DNA/RNA damage; Sulfanyl-Sulfinyl-Sulfonyl groups; synthesis of 4-thioalkylquinoline
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Funding
- France-Venezuela PCP program [2013000438]
- University of Bordeaux
- Centre National de la Recherche Scientifique (CNRS)
- Czech Ministry of Education, Youth and Sports [CZ-OPENSCREEN-LM2018130, EATRIS-CZLM2018133]
- Escuela de Medicina UEES [2022-MED-001]
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Some sulfanyl and sulfinyl derivatives exhibited lower cytotoxicity for cancer cell lines compared to sulfonyl N-oxide derivatives. Compound 81 showed pronounced selectivity for human colorectal cancer cells and leukemia cell lines.
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 x 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.
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