Synthetic approaches for sulfur derivatives containing 1,2,4-triazine moiety: their activity for in vitro screening towards two human cancer cell lines.

Abstract

A series of sulfur 1,2,4-triazine derivatives were prepared and evaluated as anticancer compounds for two human breast cancer cell lines (MCF-7, MDA-MB-231) with some of them acting as low micromolar inhibitors. Evaluation of the cytotoxicity using a 3-(4,5-dimethylthiazol-2-yl)-3,5-diphenyltetrazolium bromide (MTT) assay, the inhibition of [(3)H]thymidine incorporation into DNA, and collagen synthesis inhibition demonstrated that these products exhibit cytotoxic effects on these breast cancer cell lines in vitro. The most effective were disulfide and sulfenamide compounds with two valence sulfur atoms. A structure-activity relationship study was performed using X-ray analysis and theoretical calculations at an ab initio density functional theory (DFT) level.

• Authors: Zbigniew Karczmarzyk, Waldemar Wysocki, Zofia Urbańczyk-Lipkowska, Przemysław Kalicki, Anna Bielawska, Krzysztof Bielawski, Justyna Ławecka
• Journal: Chemical & pharmaceutical bulletin (Chem Pharm Bull (Tokyo)) Vol. 63 Issue 7 Pg. 531-7 ( 2015) ISSN: 1347-5223 [Electronic] Japan
• PMID: 26133068 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Triazines
• 1,2,4-triazine
• Sulfur

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Cell Survival (drug effects)
• Crystallography, X-Ray
• Humans
• MCF-7 Cells
• Molecular Conformation
• Quantum Theory
• Structure-Activity Relationship
• Sulfur (chemistry)
• Triazines (chemistry)