Method of inhibiting the expression of a multi-drug resistance genes and inhibiting the production of proteins resulting from the expression of such genes thereby enhancing the effectiveness of chemot
A gene expression and drug resistance technology, applied in the field of cancer treatment, can solve the problems of clinical reversal limitation of resistance, worsening patient prognosis, and binding chemotherapy, etc.
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Embodiment 1
[0225] Example 1 - A Cholesterol Absorption Inhibitor as described herein: Preparation of ascorbyl stanolyl phosphate referred to herein as "FM-VP4";
[0226] Step 1: Protect Ascorbic Acid
[0227] Fuming sulfuric acid (24%, 8.3g) was added dropwise to acetone (50ml). Ascorbic acid (12 g) was introduced into the mixture at 0°C, and the reaction mixture was stirred at 0°C for 6 hours. The resulting crystals were filtered with suction, and the filter cake was pressed dry and washed with acetone (30 ml). The product, 5,6-isopropylidene ascorbic acid (14 g) was obtained.
[0228] Step 2: Linking to Phytostanols
[0229] At 0°C, a solution of phytostanol mixture (24g) (camesteranol: 36.4%; sitostanol: 62.3%) in toluene (500ml) and pyridine (25ml) was added dropwise to phosphorus oxychloride ( 9ml) in a mixture in toluene (200mol). The mixture was stirred at room temperature for 3 hours. Pyridine hydrochloride was filtered off, and the mother liquor was concentrated to recover...
Embodiment 2
[0232] Example 2: - a kind of cholesterol absorption inhibitor described in the text: preparation of disodium ascorbyl phosphate of dehydroepiandrosterone
[0233] Acetone (150 ml) and L-ascorbic acid (50 g) were added to a dry round bottom flask at 0°C. Acetyl chloride (7.5ml) was added dropwise via addition funnel over 10 minutes. The reaction mixture was stirred at 0 °C for 24 hours. The precipitate was filtered off and washed with acetone (3 x 20ml). The white product, 5,6-isopropylidene ascorbic acid, was dried under vacuum for 1.5 hours to obtain a dry powder (52 g), yield 85%.
[0234] A dry three-neck round bottom flask was equipped with a stir bar, argon inlet and addition funnel. A solution of dehydroepiandrosterone (1.73 g, 6 mmol) in anhydrous THF (15 ml) and pyridine (2.4 ml) was added dropwise to anhydrous THF (12 ml) and POCl at 0 °C over 10 minutes 3 (0.7ml, 7.5mmol) in a mixture. A white precipitate formed immediately. The suspension was stirred for 40 m...
Embodiment 3
[0238] Example 3 - Another cholesterol absorption inhibitor described herein: Synthesis of disodium ascorbyl phosphate of 5α-androstane-3β-ol-17-one
[0239] To a dry round bottom flask was added 5α-androstane-3β-ol-17-one (1.0 g, 3.4 mmol), THF (8.6 ml) and pyridine (1.38 ml). The mixture was stirred at room temperature until a clear solution was obtained. Into another dry round bottom flask was added THF (6.9ml) and POCl 3 (0.4ml, 4.25mmol), stirred at 0°C for 5 minutes. To this mixture was added dropwise the 5α-androstane-3β-ol-17-one solution prepared above under an argon atmosphere over 10 minutes. After the addition was complete, the white suspension was stirred at 0°C for 35 minutes and at room temperature for 2 hours. The reaction was stopped and the white suspension was used for the coupling reaction without filtration.
[0240] 5,6-Isopropylidene ascorbic acid (2.0 g, 9.52 mmol) was dissolved in pyridine (1.71 ml) and THF (17 ml). The round bottom flask containi...
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