Zhu Taofeng, Shen Shanshan, Lu Qin, Ye Xingpei, Ding Weiliang, Chen Ruhua, Xie Jing, Zhu Wenjiao, Xu Jun, Jia Lei, Wu Weina, Ma Tieliang
Department of Respiratory Disease, The First Affiliated Hospital of Soochow University, Suzhou, Jiangsu 215006, P.R. China.
Department of Respiratory Disease, The Affiliated Yixing Hospital of Jiangsu University, Yixing, Jiangsu 214200, P.R. China.
Oncol Lett. 2017 Jun;13(6):4493-4500. doi: 10.3892/ol.2017.5995. Epub 2017 Apr 5.
A series of N(4)-substituted thiosemicarbazones (TSCs) bearing pyrrole unit (1a-1e) were synthesized and fully characterized by elemental analyses, infrared spectra, H nuclear magnetic resonance and single crystal X-ray diffraction. The compounds were assessed as potential chemotherapeutic agents. All newly synthesized compounds were screened for their anticancer activity against lung cancer PC-9, esophageal cancer Eca-109 and gastric cancer SGC-7901 cell lines. The results of MTT, Terminal deoxynucleotidyl transferase dUTP nick end labeling and fluorescence-activated cell sorting assays indicated that all the prepared compounds exhibited cytotoxicity against PC-9, Eca-109 and SGC-7901 cells . All the compounds significantly induced cancer cell apoptosis accompanied by increasing the Bax/Bcl-2 ratio and activation of caspase-3. The structure-activity association was discussed and the potential pre-clinical trials may be conducted. The present findings have a great potential in biomedical applications of novel N(4)-substituted TSCs.
合成了一系列带有吡咯单元的N(4)-取代硫代氨基脲（TSCs，1a - 1e），并通过元素分析、红外光谱、氢核磁共振和单晶X射线衍射对其进行了全面表征。这些化合物被评估为潜在的化疗药物。对所有新合成的化合物针对肺癌PC - 9、食管癌Eca - 109和胃癌SGC - 7901细胞系的抗癌活性进行了筛选。MTT、末端脱氧核苷酸转移酶dUTP缺口末端标记和荧光激活细胞分选分析结果表明，所有制备的化合物对PC - 9、Eca - 109和SGC - 7901细胞均表现出细胞毒性。所有化合物均显著诱导癌细胞凋亡，同时伴随着Bax/Bcl - 2比值的增加和caspase - 3的激活。讨论了构效关系，并可能进行潜在的临床前试验。目前的研究结果在新型N(4)-取代TSCs的生物医学应用方面具有巨大潜力。
