94441-01-7Relevant academic research and scientific papers
Steroid purine nucleoside analogue containing 1,2,3-triazole as well as preparation method and application thereof
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Paragraph 0032; 0033; 0034, (2017/10/22)
The invention belongs to the technical field of medical chemistry and relates to a steroid purine nucleoside analogue containing 1,2,3-triazole as well as a preparation method and application thereof. The steroid purine nucleoside analogue has a following general formula: the formula is shown in the description. The steroid purine nucleoside analogue is prepared by taking 3beta-hydroxy-5alpha-androstan-17-ketone or 4-aza-5alpha-androstan-3,17-dione as a raw material through bromination, oxidization, azidation and cycloaddition reaction; the preparation method is simple and has moderate conditions; the total yield of targets reaches 75 percent or more. The compound provided by the invention has a remarkable inhibition effect on cell lines of prostatic carcinoma, gastric carcinoma and the like and a leading compound structure is provided for further research of anti-cancer medicines, so that the variety of the steroid purine nucleoside analogue is enriched.
Synthesis, characterization and biological evaluation of some 16β-azolyl-3β-amino-5α-androstane derivatives as potential anticancer agents
Guo, Hao,Zhang, Guolan,Zhang, Tao,He, Xianran,Wu, Zhongyuan,Xiao, Yuling,Pan, Yuanhu,Qiu, Guofu,Liu, Peng,Hu, Xianming
experimental part, p. 3662 - 3674 (2011/11/05)
A series of new 16β-azolyl-3β-amino-5α-androstane derivatives were synthesized and characterized. The new compounds were screened for their anticancer activity against the human cancer cell lines SW480, A549, HepG2, HeLa and SiHa in vitro using the MTT assay. The results of the in vitro study showed that a number of compounds have shown IC50 values lower than 20 μM against the five cancer cell lines.
Synthesis and neuromuscular blocking activity of 16β-piperidino epiandrosterone derivatives
Dubey, Sonal,Jindal,Piplani, Poonam,Young, Louse C.,Fathi, Behrooz,Harvey, Alan L.
, p. 229 - 240 (2007/10/03)
This study reports the synthesis of steroidal quaternary ammonium compounds 11 and 12, with quaternary nitrogen at position 3 and 16 of the steroid nucleus in 5α-epiandrosterone series; along with their neuromuscular blocking activity using chick biventer cervicis muscle preparation. The compound 12 was found to be five times more potent than 11 in reducing twitch response to nerve stimulations, indicating the importance of extended interonium distances and 17-acetoxy function for potent antagonist activity. Birkhaeuser Boston 2006.
