846-45-7Relevant articles and documents
Structure-activity relationship and mechanistic study on guggulsterone derivatives; Discovery of new anti-pancreatic cancer candidate
Kohyama, Aki,Kim, Min Jo,Yokoyama, Rei,Sun, Sijia,Omar, Ashraf M.,Phan, Nguyen Duy,Meselhy, Meselhy R.,Tsuge, Kiyoshi,Awale, Suresh,Matsuya, Yuji
, (2021/12/24)
Pancreatic cancer is one of the deadliest types of malignancies. A new intervention aiming to combat pancreatic cancer is targeting its extra-ordinary ability to tolerate nutrition starvation, a phenomenon known as “Austerity”. As a part of a research program aiming to develop a new-generation of anticancer agents, known as “anti-austerity agents”, guggulsterone derivatives (GSDs) were identified as unique anti-austerity agents in terms of potency and selectivity. These agents are able to exert preferential cytotoxic activity only under nutrient-deprived conditions with little or no toxicity under normal conditions. In the present study, a library of 14 GSDs was synthesized and screened against PANC-1 human pancreatic cells. Among tested compounds, GSD-11 showed the most potent activity with PC50 a value of 0.72 μM. It also inhibited pancreatic cancer cell migration and colony formation in a concentration-dependent manner. A mechanistic study revealed that this compound can inhibit the activation of the Akt/mTOR signaling pathway. Therefore, GSD-11 could be a promising lead compound for the anticancer drug discovery against pancreatic cancer.
Ruthenium acetate complexes as versatile probes of metal-ligand interactions: Insight into the ligand effects of vinylidene, carbene, carbonyl, nitrosyl and isocyanide
Welby, Christine E.,Eschemann, Thomas O.,Unsworth, Christopher A.,Smith, Elizabeth J.,Thatcher, Robert J.,Whitwood, Adrian C.,Lynam, Jason M.
experimental part, p. 1493 - 1506 (2012/06/16)
Reaction of cis-Ru(2-OAc)2(PPh3) 2 with two-electron donor ligands L results in the formation of complexes trans-[Ru(1-OAc)(2-OAc)L(PPh3) 2] (L = CO, NO+, CNtBu). Vinylidene complexes (L = C=CHR) may be prepared from the corresponding reaction with terminal alkynes HC=CR, and species containing hydroxyvinylidene ligands (L = C=CHCR1R 2{OH}) may be prepared from related reactions with propargyl alcohols HC=CCR1R2{OH}. Treatment of cis-Ru(κ2- OAc)2(PPh3)2 with ω-alkynols HC=C(CH 2)nOH (n = 2-4) results in the formation of oxacyclocarbene complexes [L = CCH2(CH2)nO]. An analysis of the spectroscopic data and the structural metrics (as determined by X-ray crystallography) of this series of complexes allows for the relative donor/acceptor properties of the ligand L to be evaluated. This comparison indicates that the vinylidene ligand behaves in a similar fashion to the isocyanide ligand. The complex cis-[Ru(2-OAc)2(PPh 3)2] acts as a precursor for the formation of the complexes trans-[Ru(1-OAc)(2-OAc)L(PPh3) 2] where L is a two-electron donor, σ-donor/π-acceptor ligand. The structural and spectroscopic data of these species provide insight into the relative electron demand of the ligands L.
17-Methyleneandrostan-3alpha-ol analogs as CRH inhibitors
-
, (2008/06/13)
17-Methyleneandrostan-3α-ol analogs are useful as corticotropin releasing hormone (CRH) inhibitors, and especially as anti-depressants, when administered to the vomeronasal organ. An improved synthesis of 17-methylenandrost-4-en-3α-ol is disclosed.
