Synthesis, characterization and cytotoxic activity evaluation of ginsengdiol oxidation and nitrogen hybrid derivatives†,RSC Medicinal Chemistry

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Synthesis, characterization and cytotoxic activity evaluation of ginsengdiol oxidation and nitrogen hybrid derivatives†
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2018-10-18 00:00:00 , DOI: 10.1039/c8md00387d
Yumeng Zhang ₁ , Weihui Yuan ₁ , Xude Wang ₁ , Hongyu Zhang ₁ , Yuanyuan Sun ₁ , Xiaoshu Zhang _{1,

2} , Yuqing Zhao _{1,

2}

Affiliation

Panaxadiol (PD), a diol-type ginseng saponin, with a dammarane skeleton plays a potential role in the apoptosis of tumor cells. In this study, 28 oxidation and nitrogen hybrid derivatives of PD were synthesized, of which 20 were novel compounds. All the obtained compounds were screened for their cytotoxic activity in six cell lines. As compared with the positive control, some compounds showed better anti-proliferative activities while having much weaker effect on the growth of normal cells. Among them, ring-A fused pyrazoline of PD (1j) displayed impressive cytotoxic activity with IC₅₀ 9.62 ± 1.34, 11.65 ± 1.71, and 13.45 ± 1.60 μM against A549, HeLa and 8901 cell lines, respectively. Additionally, compound 2f exhibited the most potent activity with an IC₅₀ value of 8.93 ± 1.11 μM against cell line A549. Therefore, our results indicated that 1j and 2f can be promising lead candidates for further studies.

中文翻译：

人参二醇氧化和氮杂化衍生物的合成、表征和细胞毒活性评价†

Panaxadiol (PD) 是一种二醇型人参皂甙，具有达玛烷骨架，在肿瘤细胞凋亡中发挥潜在作用。本研究合成了 28 种 PD 的氧化氮杂化衍生物，其中 20 种为新型化合物。在六种细胞系中筛选所有获得的化合物的细胞毒活性。与阳性对照相比，一些化合物表现出更好的抗增殖活性，但对正常细胞生长的作用却要弱得多。其中，环 A 融合的 PD ( 1j ) 显示出令人印象深刻的细胞毒活性，对 A549、HeLa 和 8901 细胞系的 IC ₅₀分别为 9.62 ± 1.34、11.65 ± 1.71 和 13.45 ± 1.60 μM。此外，化合物2f表现出最强的活性，具有 IC_{对细胞系 A549 的50}值为 8.93 ± 1.11 μM。因此，我们的结果表明， 1j和2f可以成为进一步研究的有希望的主要候选者。

更新日期：2018-10-18

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