当前位置: X-MOL 学术Bioorg. Med. Chem. Lett. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis of guggulsterone derivatives as potential anti-austerity agents against PANC-1 human pancreatic cancer cells.
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-01-11 , DOI: 10.1016/j.bmcl.2020.126964
Aki Kohyama 1 , Rei Yokoyama 1 , Dya Fita Dibwe 2 , Sahar El-Mekkawy 3 , Meselhy R Meselhy 4 , Suresh Awale 2 , Yuji Matsuya 1
Affiliation  

E- and Z-guggulsterones and nine guggulsterone derivatives (GSDs) were synthesized and evaluated for their preferential cytotoxicity against human PANC-1 cell in nutrient deprived medium utilizing antiausterity strategy. Among the synthesized compounds, GSD-1 and GSD-7 showed potent cytotoxicity against PANC-1 cells under nutrient-deprived conditions in a concentration dependent manner, with a PC50 value of 1.6 μM and 3.2 μM, respectively. The effect of GSD-1 and GSD-7 was further evaluated in a real time using live cell imaging. Both of these compounds altered PANC-1 cell morphology, leading to cell death at sub micromolar concentration range. GSD-1 and GSD-7 also inhibited PANC-1 cell colony formation in a concentration-dependent manner. GSD-1 and GSD-7 are lead structure for the anti-austerity drug development.

中文翻译:

guggulsterone衍生物的合成,作为针对PANC-1人胰腺癌细胞的潜在抗紧缩药。

合成了E-和Z-古古甾酮以及九种古古甾酮衍生物(GSD),并利用抗紧缩策略评估了在营养缺乏的培养基中它们对人PANC-1细胞的优先细胞毒性。在合成的化合物中,GSD-1和GSD-7在营养缺乏的条件下以浓度依赖的方式对PANC-1细胞表现出强大的细胞毒性,其PC50值分别为1.6μM和3.2μM。使用活细胞成像进一步实时评估了GSD-1和GSD-7的作用。这两种化合物都改变了PANC-1细胞的形态,导致亚微摩尔浓度范围的细胞死亡。GSD-1和GSD-7还以浓度依赖的方式抑制PANC-1细胞集落的形成。GSD-1和GSD-7是抗紧缩药物开发的先导结构。
更新日期:2020-01-13
down
wechat
bug