1232-19-5Relevant academic research and scientific papers
Disturbance in sex-steroid serum profiles of cattle in response to exogenous estradiol: A screening approach to detect forbidden treatments
Regal, Patricia,Nebot, Carolina,Díaz-Bao, Mónica,Barreiro, Rocio,Cepeda, Alberto,Fente, Cristina
, p. 365 - 375 (2011)
Estradiol benzoate (EB) has been one of the most widely used estrogenic agents in animal husbandry, as a way of exogenously introducing the natural hormone estradiol-17β into the animal organism. Estradiol was previously employed to induce anabolic effects or reproductive improvements in cattle. However, the employment of EB in European countries has been permanently forbidden by Directive 2008/97/EC to guarantee consumers' health. Despite this prohibition, the control of estradiol-17β and its esters continues to be a difficult task for residue-monitoring plans in European Communities because official analyses of natural thresholds for hormones in cattle have not yet been established, leading to a lack of confirmation for any exogenous administration of natural hormones. Several researchers have worked on excretion profiles of metabolites, variation in specific hormonal ratios and metabolomic fingerprints after hormonal treatments. This research focuses on the possible existence of disturbances in the serum profile of animals treated with EB in terms of steroid sex hormones (androgens, oestrogens and progestogens), by investigating the serum levels of several of these hormones. The serum samples were collected from three groups of cows: one treated with an intramuscular injection of EB, one treated with a combination of intravaginal EB and progesterone and a control (non-treated) group. The samples have been analysed by a validated high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method, and 17 natural hormones were identified and quantified. Subsequently, data from the serum profiles were submitted for statistic and multivariate analysis, and it was possible to observe a manifest variation between animal groups. The obtained results can help in the development of a viable screening tool for monitoring purposes in cattle.
Synthesis and antiproliferative evaluation of novel steroid-benzisoselenazolone hybrids
Cui, Jianguo,Wei, Meizhen,Pang, Liping,Gan, Chunfang,Xiao, Junan,Shi, Haixin,Zhan, Junyan,Liu, Zhiping,Huang, Yanmin
, (2019/10/04)
The two different types of steroidal benzisoselenazolone hybrids were synthesized by incorporating benzisoselenazolone scaffold into dehydroepiandrosterone and B-norcholesterol. The antiproliferative activity of the synthesized compounds against some carcinoma cell lines were investigated. The results showed that some of these compounds have better inhibitory activity than abiraterone on the proliferation of tumor cells associated with human growth hormone, and have less cytotoxicity on normal human cells. In particular, the IC50 values of the compound 8a and 8f are 5.4 and 6.5 μmol/L against human ovarian carcinoma (SKOV3) cell line, and possess SI values of 13.9 and 10.5, respectively. The information obtained from the studies may be useful for the design of novel chemotherapeutic drugs.
A process for the production of acetate (by machine translation)
-
Paragraph 0018; 0019, (2018/09/08)
The invention belongs to the technical field of pharmaceutical and chemical industries, and in particular relates to a process for the production of acetate, this invention has improved the acetate synthetic route, to the dehydroepiandrosterone as raw materials, by condensation with hydrazine hydrate, iodo, with 3 - pyridine [...] coupled reactions, such as the acetylation 4 step reaction synthesizes the target product acetate, the overall yield is 51.4%. Is determined synthetic compound 17 - (3 - pyridyl) - androst - 5, 16 - diene - 3 β - ol the best reaction time and the reaction temperature is 5 h, 35 °C. The route mild reaction conditions, raw materials are cheap and easy to obtain, and the production cost is low. (by machine translation)
Compound with anti-tumor activity and application of compound
-
Paragraph 0033; 0034; 0035, (2016/10/10)
The invention discloses an amino-acid-oriented steroid small peptide compound with anti-tumor activity.The structure of the compound is shown in the general formula I.Corresponding hydrazone and oxime are synthesized with dehydroepiandrosterone (DHEA), DHEA and an amino acid derivative are then condensed, and the compound is obtained.The compound has a remarkable inhibiting effect on growth of tumor cells especially human hepatoma cells, human lung cancer cells and human melanoma cells, and can serve as an active ingredient for anti-tumor medicine to be applied to prevention and treatment of cancer.
17-Oximino-5-androsten-3β-yl esters: Synthesis, antiproliferative activity, acute toxicity, and effect on serum androgen level
Dhingra, Neelima,Bhardwaj, Tilak Raj,Mehta, Neeraj,Mukhopadhyay, Tapas,Kumar, Ashok,Kumar, Manoj
scheme or table, p. 817 - 825 (2012/05/04)
The 17-oximino-5-androsten-3β-yl esters (10a- 10j) 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 prostate specific cancer cell line DU-145, acute toxicity, and effect on serum androgen level and were compared with Finasteride used as positive control. Some of the compounds exhibited better cytotoxicity and antiandrogenic activity than the reference control. The detailed synthesis, spectroscopic data, and biological evaluation for the synthesized compounds are reported. Springer Science+Business Media, LLC 2010.
NOVEL STEROIDAL ESTERS OF 17-OXIMINO-5-ANDROSTEN-3BETA-OL
-
Page/Page column 2-3, (2010/12/18)
The present invention relates to steroidal esters of 17-oximino-5-androsten-3-ol, of compound of general formula (A) wherein R is selected from a group consisting of arylalkyl, aryl, substituted aryl. The ester derivatives are synthesized starting from De
NOVEL STEROIDAL ESTERS OF 17-OXIMINO-5-ANDROSTEN-3β-OL
-
Page/Page column 7, (2009/04/25)
The present invention relates to steroidal esters of 17-oximino -5-androsten-3-ol,of compound of general formula A wherein R is selected form a group consisting of arylalkyl, aryl, substituted aryl. The ester derivatives are synthesized starting from Dehy
Structure-activity relationship study of androstene steroids with respect to local anti-inflammatory activity
Chaubal, Rohini,Mujumdar, Arvind M.,Misar, Ashwini,Deshpande, Vishnu H.,Deshpande, Nirmala R.
, p. 394 - 398 (2007/10/03)
A sex hormone, 37β-acetoxy-17β-hydroxy-androst-5-ene (1) (CAS 1639-43-6), was isolated from aerial parts of Acacia nilotica. This compound is reported to have anti-inflammatory activity. In view of this, considering this molecule as a lead molecule different androstene compounds were synthesized to study their potency and structure-activity relationship with respect to local anti-inflammatory activity. The experiments indicated that 17 ketonic compounds were more active towards inflammation than their oxime analogues. Similarly, for the compounds containing an acetyl group fixed at C-3 position a decreasing trend of activity was observed in the order of ketonic, hydroxyl, oxime and acetyl group, respectively, when these groups are at C-17 position. ECV · Editio Cantor Verlag, Aulendorf.
