Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2020-11-19 , DOI: 10.1007/s11094-020-02274-z K. Kucukoglu , H. I. Gul , H. Sakagami
N,N'-bis[(1-aryl-3-heteroaryl)propylidene]hydrazine dihydrochlorides, P1, P4 – P8, and R1 – R7, were assayed against human oral squamous cell carcinoma (HSC-2, HSC-3, HSC-4), human promyelocytic leukemia cell line (HL-60), and human normal oral cells (HGF, HPC, and HPLF) as non-tumor cells to evaluate their cytotoxic properties. Peplomycin was used as a reference compound. It was found that P- and R-series hydrazone compounds exhibited cytotoxicity in a range of 11 ± 0.68 – 300 ± 1.0 ± M. Compound P1 which is a non-substituted hydrazone containing piperidine ring and compound R2 which is a 4-methyl hydrazone derivative containing pyrrolidine ring showed the most potent cytotoxic activity. These hydrazone compounds may serve as promising candidates for further studies.
中文翻译:
N,N'-双[(1-芳基-3-杂芳基)亚丙基]肼二盐酸盐的细胞毒性评价
N,N- ' -双[(1-芳基-3-杂芳基)亚丙基]肼二盐酸盐,P1,P4 - P8,和R1 - R7,分别针对人口腔鳞状细胞癌测定(HSC-2,HSC-3,HSC -4),人类早幼粒细胞白血病细胞系(HL-60)和人类正常口腔细胞(HGF,HPC和HPLF)作为非肿瘤细胞来评估其细胞毒性。霉素用作为参考化合物。已发现P系列和R系列化合物在11±0.68 – 300±1.0±M的范围内表现出细胞毒性。化合物P1是含有哌啶环的非取代和化合物R2含有吡咯烷环的4-甲基衍生物具有最强的细胞毒活性。这些化合物可作为有希望的进一步研究的候选物。