2080-86-6Relevant academic research and scientific papers
Activity of steroid 4 and derivatives 4a–4f as inhibitors of the enzyme 5α-reductase 1
Arellano, Yazmín,Bratoeff, Eugene,Heuze, Yvonne,Bravo, Marisol,Soriano, Juan,Cabeza, Marisa
, p. 4058 - 4064 (2018)
It is known that the growth of prostate metastatic bone tumor depends on androgens, and tumor formation can start from migratory malignant cells produced in that organ. These cells exhibit grater type 1 5α-reductase (5α-R1) activity than type 2 5α-reducta
Method for preparing abiraterone acetate
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Paragraph 0103-0105; 0109-0112; 0139-0145, (2020/07/14)
The invention provides a method for preparing abiraterone acetate. Specifically, the invention relates to an improved method for synthesizing abiraterone or a derivative thereof through a key 3 beta-benzoyloxy intermediate. According to the process, intermediate DHEA 3-benzoyloxy ester is a solid, the intermediate with higher purity can be obtained through a crystallization method, and the processoperability is high. Meanwhile, benzoyl is strong in electric negative force, easy to react with hydroxyl and high in acylation rate, and a six-membered ring structure is twisted in a space structureof a benzoyl functional group, so that elimination reaction is not easy to perform, and generation of process byproducts is effectively avoided.
Cytotoxic effect of novel dehydroepiandrosterone derivatives on different cancer cell lines
Garrido, Mariana,Cabeza, Marisa,Cortés, Francisco,Gutiérrez, José,Bratoeff, Eugene
, p. 301 - 311 (2013/10/01)
The aim of this study was to determine the cytotoxic effect of human cancer cells on three series of novel dehydroepiandrosterone derivatives containing triazole or pyrazole rings at C-17 and an ester moiety at C-3 of the androstane skeleton. The panel ca
In vivo and in vitro effect of androstene derivatives as 5α-reductase type 1 enzyme inhibitors
Bratoeff, Eugene,Sanchez, Araceli,Arellano, Yazmin,Heuze, Yvonne,Soriano, Juan,Cabeza, Marisa
, p. 1247 - 1254 (2013/12/04)
The aim of these studies was to synthesize twelve ester derivatives of dehydroepiandrosterone with therapeutic potential. The effect of 1-12 was demonstrated in the flank organs of gonadectomized hamsters treated with testosterone and the synthesized ster
Synthesis and Antitumor Activity of Dehydroepiandrosterone Derivatives on Es-2, A549, and HepG2 Cells in vitro
Liu, Xue-Kun,Ye, Bai-Jun,Wu, Yan,Nan, Ji-Xing,Lin, Zhen-Hua,Piao, Hu-Ri
experimental part, p. 523 - 529 (2012/06/15)
A series of dehydroepiandrosterone derivatives containing an acid ester was synthesized and evaluated for their antitumor activity on ES-2, A549, and HepG2 cells by the MTT assay. Most compounds showed antitumor activity, while compounds 1c, 2i, and 2o exhibited more potential inhibitory effects compared with dehydroepiandrosterone on ES-2 cells, A549 cells, and HepG2 cells, respectively.
Synthesis, antiproliferative activity, acute toxicity and assessment of the antiandrogenic activities of new androstane derivatives
Dhingra, Neelima,Bhardwaj,Mehta, Neeraj,Mukhopadhyay, Tapas,Kumar, Ashok,Kumar, Manoj
experimental part, p. 1055 - 1063 (2012/07/28)
A number of 17-oxo-5-androsten-3β-yl esters (9a-9f) and 3β-alkoxy-5-androsten-17-ones (11a-11e) were synthesized from commercially available (25R)-5-spirosten-3β-ol (Diosgenin) (4) as starting material. The synthesized compounds were evaluated for their antiproliferative activity against the prostate-specific cancer cell line DU-145, acute toxicity and effect on serum androgen levels, and compared with finasteride as positive control. Some of the compounds exhibited better cytotoxicity and antiandrogenic activity than the reference control. The detailed synthesis, spectroscopic data and biological activity of the synthesized compounds are reported.
Action de l'anhydride acetique et des chlorures de benzoyle et de p-toluene sulfonyle sur des nitrones derivees de ceto-17 steroides. Conditions conduisant a un rearrangement ou a une fonctionnalisation
Cherest, M.,Lusinchi, X.
, p. 227 - 232 (2007/10/02)
The reaction of the title reagents under anhydrous conditions and in the presence of base leads to steroidal derivatives functionalised at position 16; whereas, in the presence of water, paratoluenesulphonyl chloride gives 17-aza-D-homo lactams by ring expansion, and use of benzoyl chloride promotes a hydrolytic fragmentation.In contrast to earlier studies, the formation of an oxaziridine under aqueous alkaline conditions was not observed in this work.These results, when considered in conjunction with those previously obtained, enable the course of these reactions to be determined as a function of the reaction conditions.
