Discovery of 2-pyridineformamide thiosemicarbazones as potent anti austerity agents.

Discovery of 2-pyridineformamide thiosemicarbazones as potent anti austerity agents.
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发现 2-吡啶甲酰胺缩氨基硫脲作为有效的抗紧缩剂。

DOI:
10.1016/j.bmcl.2013.12.044
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发表时间:
2014
期刊:
Bioorg. Med. Chem. Lett.
影响因子:
--
通讯作者:
Awale S.
Awale S.
中科院分区:
--
文献类型:
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作者:
Shakya B.;Yadav P.N.;Ueda J.;Awale S.

文献摘要

相似文献

合成了系列2-吡啶甲酰胺缩氨基硫脲。通过采用反紧缩策略,使用 PANC-1 人胰腺癌细胞评估了它们在营养剥夺培养基 (NDM) 中的优先细胞毒性。 2-吡啶甲酰胺缩氨基硫脲可诱导细胞凋亡,并对 NDM 中的 PANC-1 细胞表现出优先的细胞毒活性,效力在亚微摩尔范围内。这些化合物是开发胰腺癌疗法的潜在候选者。
Series of 2-pyridineformamide thiosemicarbazones were synthesized. Their preferential cytotoxicity in nutrient deprived medium (NDM) was evaluated using PANC-1 human pancreatic cancer cells by employing an antiausterity strategy. 2-Pyridineformamide thiosemicarbazones induced apoptosis and exhibited preferential cytotoxic activity toward PANC-1 cells in NDM, with potencies in the submicromolar range. These compounds are potential candidates for the development of therapeutics against pancreatic cancer.