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A kind of triptolide derivative and its preparation method and application
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A technology of triptolide and coumarin derivatives, which is applied in the field of medicine, can solve the problems such as the inability to maintain drug activity, toxic and side effects, and achieve the effects of reducing toxicity, reducing toxic and side effects, and improving selectivity.
Active Publication Date: 2019-04-02
HUBEI UNIV
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[0004] The current research is mainly to modify the structure of triptolide to its structural analogues, or use triptolide as a lead compound to modify the structure of triptolide through a prodrug strategy, although the drug’s Water-soluble, but still not a good solution to reduce its toxic side effects while maintaining drug activity
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Embodiment 1
[0031]
[0032] (1) After mixing 1.0g (6.58mmol) of hydroquinone and 0.54g (7.50mmol) of acrylic acid, add it to 10mL of methanesulfonic acid at one time, heat and stir at 70°C for 18h, TLC detects that the reaction is complete, stop stirring, and add 125mL of water, It was extracted with ethyl acetate successively, washed with water, saturated aqueous sodiumbicarbonate solution and saturated brine, dried over anhydroussodiumsulfate, and evaporated to dryness under reduced pressure. Recrystallized from chloroform-n-hexane to obtain a white solid, namely compound CX-11, with a yield of about 67%. [M+H] + :207.0; 1 H NMR,600MHz(CDCl3)δ4.13(bs,1H),2.92(t,2H),2.72(t,2H),2.22(s,3H),2.19(s,3H),2.18(s,3H) .
[0033]
[0034] (2) 1.39g (6.74mmol) of CX-11 was dissolved in 15mL of acetonitrile and 3mL of water; 1.26g (7.08mmol) of NBS was added to the above solution several times, stirred in an ice bath for 5min, and then evaporated to dryness under reduced pressure. The r...
Embodiment 2
[0038]
[0039] (1) Mix 1.0g (6.58mmol) hydroquinone and 0.85g (7.50mmol) 3-methyl-2-butenoic acid, add it to 10mL methanesulfonic acid at one time, heat and stir at 70°C for 4h, and detect the reaction by TLC Completely, stop stirring, add 125mL of water, extract with ethyl acetate successively, wash with water, saturated aqueous sodiumbicarbonate solution and saturated brine, dry over anhydroussodium sulfate, and evaporate to dryness under reduced pressure. Recrystallized from chloroform-n-hexane to obtain a white solid, which is compound CX-21, with a yield of about 87%. [M+H] + :235.0; 1 HNMR,600MHz(CDCl3)δ4.13(s,1H),2.56(s,2H),2.35(s,3H),2.23(s,3H),2.19(s,3H),1.46(s,6H)
[0040]
[0041] (2) 1.58g (6.74mmol) of CX-21 was dissolved in 15mL of acetonitrile and 3mL of water; 1.26g (7.08mmol) of NBS was added to the above solution several times, stirred at room temperature for 30min, and then evaporated to dryness under reduced pressure. The residue was extracted wit...
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Abstract
The invention discloses a triptolide derivative as well as a preparation method and application thereof. A chemical structural formula of the triptolide derivative disclosed by the invention is shown as follows: the chemical structural formula is shown in the description, wherein R1 and R2 are H, CH3 or NH2; R3, R4 and R5 are H, CH3, NH2, OCH3 or X. According to the triptolide derivative disclosed by the invention, the toxic side effect of triptolide is reduced under the condition that the biological activity of the triptolide is kept, so that the triptolide can be safely and effectively applied in clinical practice.
Description
technical field [0001] The invention relates to the technical field of medicine, in particular to a triptolide derivative and its preparation method and application. Background technique [0002] Cancer is one of the diseases with the highest morbidity and mortality in the world, which has seriously threatened human health. Although great progress has been made in the research of anticancer drugs, long-term drug use leads to drug resistance of cancer cells. Most anticancer drugs can also harm normal cells in the human body while killing cancer cells. In addition, anticancer drugs also have a certain degree of mutagenic genotoxicity. [0003] Triptolide, also known as triptolide, is an epoxyditerpenelactone compound isolated from the Euonymus family Tripterygiumgenus. It is the main active ingredient of the traditional Chinese medicineplantTripterygium wilfordii. Inflammation, immunosuppression, anti-fertility and anti-tumor effects. Among them, the antitumor effect o...
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