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首页> 外文期刊>Archiv der Pharmazie >Synthesis, cytotoxicity, and pro-apoptosis activity of etodolac hydrazide derivatives as anticancer agents
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Synthesis, cytotoxicity, and pro-apoptosis activity of etodolac hydrazide derivatives as anticancer agents

机译：依托度酸肼衍生物作为抗癌剂的合成，细胞毒性和促凋亡活性

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Etodolac hydrazide and a novel series of etodolac hydrazide-hydrazones 3-15 and etodolac 4-thiazolidinones 16-26 were synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR, 1H NMR, 13C NMR, HREI-MS) methods. Some selected compounds were determined at one dose toward the full panel of 60 human cancer cell lines by the National Cancer Institute (NCI, Bethesda, USA). 2-(1,8-Diethyl-1,3,4,9- tetrahydropyrano[3,4-b]indole-1-yl)acetic acid[(4-chlorophenyl)methylene] hydrazide 9 demonstrated the most marked effect on the prostate cancer cell line PC-3, with 58.24% growth inhibition at 10-5 M (10 μM). Using the MTT colorimetric method, compound 9 was evaluated in vitro against the prostate cell line PC-3 and the rat fibroblast cell line L-929, for cell viability and growth inhibition at different doses. Compound 9 exhibited anticancer activity with an IC50 value of 54 μM (22.842 μg/mL) against the PC-3 cells and did not display any cytotoxicity toward the L-929 rat fibroblasts, compared to etodolac. In addition, this compound was evaluated for caspase-3 and Bcl-2 activation in the apoptosis pathway, which plays a key role in the treatment of cancer. Etodolac hydrazide and a novel series of etodolac hydrazide-hydrazones 3-15 and etodolac 4-thiazolidinones 16-26 were synthesized. 2-(1,8-Diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-yl)acetic acid[(4-chlorophenyl)methylene]hydrazide 9 demonstrated the most marked cell viability and growth inhibition effects. It was evaluated for caspase-3 and Bcl-2 activation in the apoptosis pathway.
机译：这项研究合成了乙二酰肼和一系列新的乙二酰肼-et 3-15和乙二酰4-噻唑烷酮16-26。通过光谱（FT-IR，1H NMR，13C NMR，HREI-MS）确定新化合物的结构。美国国家癌症研究所（NCI，贝塞斯达，美国）以一剂剂量对全部60种人类癌细胞系进行了测定。 2-（1,8-二乙基-1,3,4,9-四氢吡喃并[3,4-b]吲哚-1-基）乙酸[（4-氯苯基）亚甲基]酰肼9对乙酰氨基酚的影响最明显。前列腺癌细胞系PC-3，在10-5 M（10μM）时具有58.24％的生长抑制。使用MTT比色法，针对前列腺细胞系PC-3和大鼠成纤维细胞系L-929在体外评估化合物9在不同剂量下的细胞生存力和生长抑制。与依托度酸相比，化合物9表现出对PC-3细胞的抗癌活性，IC50值为54μM（22.842μg/ mL），并且对L-929大鼠成纤维细胞没有任何细胞毒性。此外，评估了该化合物在凋亡途径中的caspase-3和Bcl-2活化，这在癌症的治疗中起关键作用。合成了Etodolac酰肼和一系列新的依托度酸肼-hydr 3-15和依托度酸4-噻唑烷酮16-26。 2-（1,8-二乙基-1,3,4,9-四氢吡喃并[3,4-b]吲哚-1-基）乙酸[（4-氯苯基）亚甲基]酰肼9具有最明显的细胞活力，生长抑制作用。评价其在凋亡途径中的caspase-3和Bcl-2活化。

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