10481-80-8Relevant articles and documents
Synthesis and bioevaluation of novel steroidal isatin conjugates derived from epiandrosterone/androsterone
Ke, Shaoyong,Zhang, Zhigang,Liu, Manli,Fang, Wei,Huang, Daye,Wan, Zhongyi,Zhou, Ronghua,Wang, Kaimei,Shi, Liqiao
, p. 1607 - 1614 (2019)
Steroids are classes of natural products widely distributed in nature, which have been demonstrated to exhibit broad biological functions, and have also attracted increasing interest from bioorganic and pharmaceutical researches. In order to develop novel chemical entities as potential cytotoxic agents, a series of steroidal isatin conjugations derived from epiandrosterone and androsterone were efficiently prepared and characterized, and all these obtained compounds were screened for their potential cytotoxic activities. The preliminary bioassay indicated that most of the newly synthesized compounds exhibited good cytotoxic activities against human gastric cancer (SGC-7901), melanoma (A875), and hepatocellular liver carcinoma (HepG2) cell lines compared with 5-fluorouracil (5-FU), which might be considered as promising scaffold for further development of potential anticancer agents.
Steroid derivative containing isatin unit as well as preparation method and application thereof
-
Paragraph 0029; 0032-0034; 0037; 0040-0042, (2019/06/07)
The invention provides a steroid derivative containing an isatin unit as well as a preparation method and application thereof. The structure formula of the steroid derivative containing the isatin unit is as shown in the formula I (the formula is shown in the description). The preparation method of the compound comprises the steps that (1) a compound epiandrosterone or androsterone serves as an initial raw material to make dehydration reaction with hydrazine hydrate to obtain an intermediate; (2) the intermediate makes condensation reaction with substituation isatin in a solvent, so that a first kind of target compound with R1 being H is obtained; and (3) the first kind of target compound with R1 being H makes esterification reaction with chloride with the structure formula being R1Cl in asolvent, so that a second kind of target compound with R1 being CH3CO, CH3CH2CO, CH3SO2 or PhCO is obtained. The compound can serve as a substite product used for preparing active components of novelanticancer drugs.
Abiraterone acetate reducing impurity and preparation method thereof
-
, (2017/10/22)
The invention discloses an abiraterone acetate reducing impurity and a preparation method thereof. The impurity is 17-(3-pyridyl) androstane-3 beta-acetoxyl. The preparation method of the impurity includes the steps: taking dehydroepiandrosterone as a starting material; performing catalytic hydrogenation by palladium carbon to obtain (3 beta)-3-hydroxy-17-sterone; performing reaction by hydrazine hydrate to obtain 17-hydrazono-androstane-3 beta-alcohol; performing iodine substitution to obtain 17-iodine-androstane-3 beta-alcohol; reacting the 17-iodine-androstane-3 beta-alcohol with borane reagents under palladium catalysis to obtain 17-(3-pyridyl) androstane-3 beta-alcohol; performing acetic anhydride acetylation to obtain the abiraterone acetate reducing impurity 17-(3-pyridyl) androstane-3 beta-acetoxyl.