| Literature DB >> 32057581 |
Aki Kohyama1, Rei Yokoyama1, Dya Fita Dibwe2, Sahar El-Mekkawy3, Meselhy R Meselhy4, Suresh Awale5, Yuji Matsuya6.
Abstract
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.Entities:
Keywords: Antiausterity agent; Drug discovery; Guggulsterone; PANC-1; Pancreatic cancer; Preferential cytotoxicity; Steroid
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Year: 2020 PMID： 32057581 DOI： 10.1016/j.bmcl.2020.126964
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823