Novel synthetic aromatic thiourea derivatives and investigations on their cytotoxic potential efficacy,Journal of Heterocyclic Chemistry

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Novel synthetic aromatic thiourea derivatives and investigations on their cytotoxic potential efficacy
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-09-02 , DOI: 10.1002/jhet.4145
Ujjayinee Ray ₁ , Franklin John ₂ , Sayeesh Pooppadi ₂ , Jinu George ₂ , Shivangi Sharma ₁ , Sathees C Raghavan ₁

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Aromatic thiourea derivatives were synthesized by standard reactions from isothiocyanates in high yield. An efficient one‐pot synthesis of primary amine with carbon disulfide involving the intermediate dithiocarbamate conversion using T₃P (propane phosphonic anhydride) to isothiocyanate is reported. Newly synthesized compounds showed excellent luminescence property. Cytotoxic investigation with different human cancer cell lines showed IC₅₀ values varying from of 17 to 40 μM for N‐phenethyl‐3,4‐dihydroisoquinoline‐2(1H)‐carbothioamide (SCR172) among other molecules. Increase in Sub G1 population and increased depolarisation of mitochondria were evident in cells treated with SCR172, suggesting its role as a cancer therapeutic agent. This provides a lead structure for further synthetic modifications.

中文翻译：

新型合成芳族硫脲衍生物及其细胞毒性潜能研究

通过标准反应由异硫氰酸酯以高收率合成芳族硫脲衍生物。据报道，二硫化碳可以有效地一锅合成伯胺，包括使用T ₃ P（丙烷膦酸酐）将二硫代氨基甲酸酯中间体转化为异硫氰酸酯。新合成的化合物显示出优异的发光性能。用不同的人类癌细胞系进行细胞毒性研究显示IC ₅₀N-苯乙基-3,4-二氢异喹啉-2（1H）-碳硫代酰胺（SCR172）的值介于17至40μM之间。在用SCR172处理的细胞中，Sub G1种群的增加和线粒体去极化的增加是很明显的，这表明它是癌症治疗剂。这提供了用于进一步合成修饰的前导结构。

更新日期：2020-09-02

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