@article {204849,
	title = {Synthesis of guggulsterone derivatives as potential anti-austerity agents against PANC-1 human pancreatic cancer cells.},
	journal = {Bioorganic \& medicinal chemistry letters},
	volume = {30},
	year = {2020},
	pages = {126964},
	abstract = {<p>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 PC 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.</p>
},
	author = {Kohyama, Aki and Yokoyama, Rei and Dibwe, Dya Fita and El-Mekkawy, Sahar and Meselhy, Meselhy R and Awale, Suresh and Matsuya, Yuji}
}
