10211-88-8Relevant articles and documents
SAR studies on azasterols as potential anti-trypanosomal and anti-leishmanial agents
Gigante, Federica,Kaiser, Marcel,Brun, Reto,Gilbert, Ian H.
, p. 5950 - 5961 (2009)
There is an urgent need for the development of new drugs for the treatment of neglected tropical diseases such as human African trypanosomiasis, Chagas disease and leishmaniasis. Azasterols, have been shown to have activity against the parasites which cause these diseases. In this paper we report synthesis of new azasterols and subsequent analysis of the SAR. The chemistry focused on variations in the ester at the 3β-position of the sterol and the position of the nitrogen in the side chain. The data allowed us to derive preliminary pharmacophore models for the activity of the azasterols against the parasites which cause these diseases.
Synthesis of an isomer of antheridiol.
McMorris
, p. 458 - 460 (1970)
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Studies on steroids. LI. Stereoselective introduction of 22- and 24-hydroxyl function in the steroidal side chain
Ishiguro,Saito,Sakamoto,Ikekawa
, p. 3715 - 3721 (1978)
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Synthesis of some steroidal derivatives with side chain of 20-and 22-hydrazone aromatic heterocycles and their antiproliferative activity
Gan, Chunfang,Liu, Liang,Cui, Jianguo,Liu, Zhiping,Shi, Haixin,Lin, Qifu,Sheng, Haibing,Yang, Chunhui,Huang, Yanmin
, p. 375 - 383 (2017/06/20)
Background: The modification of steroidal structure is commonly used to change the biological activity of steroids in medicinal chemistry. Some steroids containing heterocycles exhibit distinct cytotoxicity against various cancer cell lines and have been receiving wide attention over the years by medicinal chemists for drug discovery. Methods: Using pregnenolone and stigmasterol as starting materials, via different chemical reaction, two series of heterosteroids with side chain of 20- and 22-hydrazone aromatic cycles or heterocycles in their structures were synthesized and characterized by IR, NMR and HRMS. The antiproliferative activity of the compounds in vitro was evaluated against human HT-29, HeLa, Bel 7404 and SGC 7901 cancer cells by MTT assays. Results: The steroidal compounds with side chain of 20-hydrazone aromatic cycles or heterocycles exhibited distinct cytotoxicity. However, analogues with the side chain of 22-hydrazone resulted in a dramatic decrease of the cytotoxicity. The result of Annexin V assay showed that the 20-hydrazone compounds were potent apoptotic inducers against these carcinoma cells. Conclusion: Steroidal compounds with the side-chain of 20-hydrazone aromatic heterocycles exhibit distinct antiproliferative activity in vitro. However, the compounds with the side-chain of 22-hydrazone aromatic heterocycle decreased the cytotoxicity of the compounds.
NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF
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, (2016/02/16)
Provided are methods of evaluating or treating a patient, e.g., a patient having a disorder described herein, comprising: a) optionally, acquiring a patient sample; b) acquiring an evaluation of and/or evaluating the sample for an alteration in the level S24(S)-hydroxycholesterol compared to a reference standard.
