1971-59-1Relevant academic research and scientific papers
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-catalyzed synthesis of β-oxo esters in aqueous medium: Scope and limitations
Cadierno, Victorio,Francos, Javier,Gimeno, Jose
experimental part, p. 135 - 143 (2010/05/18)
The ability of the hydrosoluble ruthenium(ii) complexes [RuCl 2(η6-arene)(PTA)] 3a-d, [RuCl2(η 6-arene)(PTA-Bn)] 4a-d, [RuCl2(η6-arene) (DAPTA)] 5a-d, [RuCl2(η6-arene)(TPPMS)] 6a-d (arene = C6H6, p-cymene, 1,3,5-C6H3Me 3, C6Me6) to promote the atom-economic formation of β-oxo esters, by addition of carboxylic acids to terminal propargylic alcohols in water has been explored. Scope, limitations and catalyst recycling have been evaluated using the most active catalyst [RuCl 2(η6-C6H6)(TPPMS)], 6a.
Studies on anabolic steroids. 9. Tertiary sulfates of anabolic 17α-methyl steroids: synthesis and rearrangement
Bi, Honggang,Masse, Robert,Just, George
, p. 306 - 312 (2007/10/02)
A simple and convenient method has been developed to prepare sulfates of anabolic 17β-hydroxy-17α-methyl steroids.The sulfates of methandienone, 17α-methyltestosterone, mestanolone, oxandrolone, and stanozolol were prepared.Different A-ring functions were not affected under the sulfation condition.The buffered hydrolyses of these sulfates provided the 17-epimers of the original steroids and 17,17-dimethyl-18-nor-13(14)-ene steroids, presumably via the 17-carbocations. Keywords: steroids, tertiary sulfates; 17α-methyl steroids; 17β-methyl steroids; 17,17-dimethyl-18-norandrost-13(14)-enes; NMR
Dermatics utilizing 17βmethyl-18 nor steroids and methods for their use
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, (2008/06/13)
Dermatics are claimed which are characterized in that they contain as the active compound one or two 17β-methyl-18-nor steroids of general Formula I STR1 wherein is a single bond or a double bond, R1 is a hydrogen atom or a methyl group, and R2 is an alkyl group of maximally 6 carbon atoms, optionally substituted by an alkanoyloxy group containing 2-6 carbon atoms.
