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A kind of puma inhibitor and its preparation method and use
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A technology of inhibitors and uses, applied in the field of medicine, to achieve the effect of blocking apoptosis, good physical and chemical properties, and good resistance to apoptosis
Inactive Publication Date: 2020-06-30
FOURTH MILITARY MEDICAL UNIVERSITY
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Problems solved by technology
[0005] Radiation-damaged drugs targeting PUMA proteins are innovative fields worldwide, with few reports in the literature
Method used
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preparation Embodiment 1
[0056]
[0057] Add 2.0 g (15 mmol) of rhodanine, 20 mL of anhydrousmethanol, and 0.1 mL of glacial acetic acid in a three-necked flask. 2 Under protection, 2.9 g (22.6 mmol) of hydroxyethylpiperazine and 22.6 mmol of benzaldehyde were added, and the oil bath was refluxed to obtain a light yellow clear reaction liquid, which was monitored by TLC in time. After 1-2 hours, the reaction was completed, and a yellow solid was precipitated in an ice bath. Suction filtration, washing with methanol, the crude product was purified by silica gelcolumn chromatography (DCM:MeOH 10:1) to obtain pure compound 1 with a yield of 35-55%.
[0058] Yellow solid, 46% yield. 1 H NMR (400MHz, CDCl 3 )δ=7.83(s,1H),δ=7.56(d,2H),δ=7.47(m,2H),δ=7.41(t,1H),δ=4.1(t,2H),δ=3.69( m, 4H), δ=2.72(t, 2H), δ=2.66(m, 4H). 13 CNMR (400MHz, CDCl 3 ) 180.84, 175.22, 134.16, 131.94, 129.78, 129.74, 129.03, 127.88, 59.26, 58.05, 52.53, 52.11, 48.68, 48.34, HRMS (ESI) calcd.for C 16 h 19 N 3 o 2 S:317.1[M...
preparation Embodiment 2
[0060] Compound 2 was prepared in the same manner as in Preparation Example 1 except that p-phenylbenzaldehyde was used instead of benzaldehyde.
[0061] Pale yellow solid, yield = 52.9%, 1 H NMR (400MHz, CDCl 3 )δ=7.87(s,1H),δ=7.69(d,2H),δ=7.63(m,4H),δ=7.48(t,2H),δ=7.42(t,1H),δ=5.32( s,1H),δ=4.1(t,2H),δ=3.71(m,4H),δ=2.73(t,2H),δ=2.68(m,4H)HRMS(ESI)calcd.for C 22 h 23 N 3 o 2 S 394.2[M+H] + ,found 394.2[M+H] + .
preparation Embodiment 3
[0063] Compound 3 was prepared in a similar manner to Preparation Example 1 except that p-tolualdehyde was used instead of benzaldehyde.
[0064] Pale yellow solid, yield = 49.1%, 1 H NMR (400MHz, CDCl 3 )δ=7.81(s,1H),δ=7.43(d,2H),δ=7.27(t,3H),δ=4.12(t,2H),δ=3.70(m,4H),δ=2.73( t,2H), δ=2.68(m,4H), δ=2.40(s,3H)HRMS(ESI)calcd.for C 17 h 21 N 3 o 2 S 331.4[M+H] + ,found 331.8[M+H] + .
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PUM
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Abstract
The present invention relates to the field of medical technology, specifically to a type of PUMA inhibitor and its preparation method and use. The PUMA inhibitor is a compound of the following formula I or a pharmaceutically acceptable salt thereof. Wherein, the definition of each substituent is as described in the specification. The compound of formula I or its pharmaceutically acceptable salt of the present invention can target PUMA protein, has good physical and chemical properties, good anti-apoptosis and radioprotective effects, and can selectively inhibit the interaction between PUMA protein and Bcl-2 class The competitive binding between anti-apoptotic proteins blocks cellapoptosis and effectively protects against bone marrow damage. The present invention provides novel ideas and strong evidence for the application of small molecule inhibitors of PUMA protein in radiation protection drugs, and is expected to become an efficient, low-toxic and stable clinical radiation protection drug.
Description
technical field [0001] The invention relates to the technical field of medicine, in particular to a class of PUMA inhibitors and a preparation method and application thereof. Background technique [0002] The rapid development of nuclear radiation technology has been widely used in many economic and military fields, such as medical diagnosis and treatment, nuclear power generation, radiation breeding, terrorist activities, nuclear war, etc. The widespread use of these nuclear energies has resulted in more and more people being exposed to high-energy ionizing radiation. Radiation can cause serious damage to the body, such as hematopoietic stem cell damage, organ lesions, radiation mutagenesis, and radiation-induced cancer. [0003] Myeloid injury is the most basic and common type of radiation injury. Immediately interrupting such injuries is the primary measure for most acute radiation protection. Starting from the mechanism of radiation injury, identifying drug targets an...
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