35882-85-0Relevant academic research and scientific papers
Sterol compound and its pharmaceutically acceptable salt or prodrug, and application thereof
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, (2019/10/01)
The present invention discloses a sterol compound and its pharmaceutically acceptable salt or prodrug, and an application thereof in the prevention or treatment of malignant tumors associated with LXR. The compound has an inhibitory ability against various malignant tumors in in-vitro experiments, and also has an inhibitory ability against malignant tumors malignant tumors in in-vivo experiments.The sterol skeleton compound has the equivalent curative effect on the malignant tumors with cytotoxic drugs currently used for treating the tumors, and has the same therapeutic effect with positive drugs for evaluating the drug effect of the compound. The compound has the advantages of good antitumor activity, good safety, no side effects caused by the positive drugs, and facilitation of enhancement of the immune function of animals. The sterol compound has a potential to become a safe and effective broad-spectrum antitumor drug.
Preparation method for 3beta-hydroxy-ergosta-5-ene steroid compound
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, (2019/02/10)
The invention provides a novel synthetic method for 3beta-hydroxy-ergosta-5-ene steroid derivative. The method includes the following steps: 1, taking stigmasterol 1-a as an initial raw material, andpreparing an intermediate aldehyde compound 1-b through multi-step reaction; 2, starting from the compound 1-b to obtain a compound 1-c through witting reaction; 3, preparing a compound 1-d from the compound 1-c through a reduction reaction; 4, obtaining a compound 1 by the compound 1-d through a nucleophilic addition reaction; and 5, preparing a 3beta-hydroxy-ergosta-5-ene steroid from the compound 1. Compared with the prior art, the method realizes the massive and efficient preparation of the compound from stigmasterol; and synthetic raw materials are easy to obtain, synthetic processes aresimple in operation, and the method is high in yield.
3beta-hydroxy-ergosta-5-ene steroid derivative and drug application thereof
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Paragraph 0033; 0043-0045, (2019/02/13)
The invention provides a structure of a 3beta-hydroxy-ergosta-5-ene steroid compound, and applications of the compound and the pharmaceutically acceptable form of chemical protection or a prodrug in the preparation of drugs capable of preventing or treating LXRbeta related metabolic syndromes. The LXRbeta related metabolic syndromes include hyperlipidemia, atherosclerosis or hypertension. Throughthe discovery of the evaluation of lipid-lowering activity in animal bodies, the compound has obvious effects on lipid lowering, so that the compound has potentials of further developing into a novellipid-lowering drug.
Structure-activity relationships of oxysterol-derived pharmacological chaperones for Niemann-Pick type C1 protein
Ohgane, Kenji,Karaki, Fumika,Noguchi-Yachide, Tomomi,Dodo, Kosuke,Hashimoto, Yuichi
supporting information, p. 3480 - 3485 (2014/07/22)
Niemann-Pick disease type C is a fatal neurodegenerative disease, and its major cause is mutations in NPC1 gene. This gene encodes NPC1 protein, a late endosomal polytopic membrane protein required for intracellular cholesterol trafficking. One prevalent mutation (I1061T) has been shown to cause a folding defect, which results in failure of endosomal localization of the protein, leading to loss-of-function phenotype. We have previously demonstrated that several oxysterols and their derivatives act as pharmacological chaperones; binding of these compounds to NPC1I1061T mutant protein corrects the localization/maturation defect of the mutant protein. Here, we disclose detailed structure-activity relationships of oxysterol derivatives as pharmacological chaperones for NPC1I1061T mutant.
NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF
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Paragraph 00373, (2013/03/26)
Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L1, L2, L3, X1, X2, Y, Rz4, Rz5, Rz6, n, R1, R2, R3a, R3b, R4a, R4b, R6a, R6b, R7a, R7b, R11a, R11b, R14, R17, R19, R20, R23a, R23b, and R24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.
Studies on vitamin D (calciferol) and its analogues. 15. 24-nor-1α,25-dihydroxyvitamin D3 and 24-nor-25-hydroxy-5,6-trans-vitamin D3
Mourino,Blair,Wecksler,Johnson,Norman,Okamura
, p. 1025 - 1029 (2007/10/17)
As part of our continuing structure-function study of the vitamin D3 (2a) endocrine system and particularly the key metabolites 25-hydroxyvitamin D3 (2b) and 1α,25-dihydroxyvitamin D3 (2c), the analogues 24-nor-1α,25-dihyd
