1971-59-1Relevant 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.
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
Influence of the steroid A ring on the reactivity at the level of carbons 13 and 14. II. The BF3-catalyzed oxirane ring opening of the 13,14-epoxy steroids in the estrone and testosterone series
Torreilles,Crastes de Paulet
, p. 4886 - 4892 (2007/10/06)
-