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Pyrazol compound and purpose of pyrazol compound used as receptor tyrosine kinases (RTK) and phosphatidyl inositol 3-kinase (PI3K) dual inhibitors
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A compound and selected technology, applied in organic chemistry, drug combination, antineoplastic drugs, etc., can solve problems such as resistance to tyrosine inhibitors
Inactive Publication Date: 2012-07-25
CHINA PHARM UNIV
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However, abnormalities in the PI3K pathway lead to resistance to receptor tyrosine inhibitors
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Embodiment 1
[0227] 3-amino-4-carboxamido-5-(2-nitrophenyl)-1-n-octyl-1H-pyrazole (III 1 ): 30 grams of 2-nitrobenzoic acid reacted with 180 milliliters of thionylchloride for 6 hours under the condition of reflux, and concentrated under reduced pressure to obtain 2-nitrobenzoyl chloride. Dissolve 30 g of malononitrile in THF, and carefully add 2 times the amount of NaH at 0°C. After the addition, react for 2 hours, add the previously prepared 2-nitrobenzoyl chloride dropwise to the above solution, and the reaction temperature does not exceed 5 degrees Celsius. After the dropwise addition was completed, the reaction was continued for 6 hours. The reaction solution was poured into ice water. Chloroform extraction, the organic phase was dried and concentrated. Add 100 ml of THF and 20 ml of water to the concentrated solution, add 60 g of potassiumcarbonate, reflux for 2 hours, concentrate under reduced pressure and carefully add 40 ml of hydrazine hydrate. After reacting at 90 degrees ...
Embodiment 2
[0229] 3-Amino-4-carboxamido-5-(2-nitrophenyl)-1-n-nonyl-1H-pyrazole (III 2 ) synthetic method with reference to the general method above: 1H NMR (DMSO, 300MHz) δ (ppm): 8.00 (d, 1H, J = 9.0Hz), 7.75 (t, 1H, J = 6.9Hz), 7.61 (t, 1H, J = 6.9Hz), 6.30 ( br, 4H), 3.86(t, 2H, J=6.0Hz), 1.62(br, 2H), 1.23(br, 12H), 0.84(t, 3H, J=6.6Hz); MS (ESI, m / z ): 374.2 (M+H) +
Embodiment 3
[0231] 3-Amino-4-carboxamido-5-(2-nitrophenyl)-1-n-decyl-1H-pyrazole (III 3 ) synthetic method with reference to the general method above: 1 H NMR (DMSO, 300MHz) δ (ppm): 8.00 (d, 1H, J = 9.0Hz), 7.75 (t, 1H, J = 6.9Hz), 7.61 (t, 1H, J = 6.9Hz), 6.30 ( br, 4H), 3.86(t, 2H, J=6.0Hz), 1.62(br, 2H), 1.23(br, 14H), 0.84(t, 3H, J=6.6Hz); MS (ESI, m / z ): 388.2(M+H) +
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Abstract
The invention provides a group of novel tyrosinekinase and phosphatidyl inositol 3-kinase (PI3K) dual inhibitors, which have higher anti-tumor activity. A preparation method for synthesizing the novel tyrosinekinase and PI3K dual inhibitors is characterized in that the novel tyrosine kinase and PI3K dual inhibitors are obtained through manual synthesis. The novel tyrosine kinase and PI3K dual inhibitors synthesized by using the method provided by the invention can be used for preparing cancer treatment medicine.
Description
technical field [0001] The present invention relates to a group of novel pyrazole compounds with pharmacological activity, their preparation method and pharmaceutical compositions containing them. Background technique [0002] Phosphatidylkinol 3-kinase (PI3-K) is an important kinase in cells (Carpenter et al, Mol. Cell. Biol. 1993, 13: 1657-1665). It participates in intracellularsignal transduction by activating Akt / PKB, MAPK, PKC and other signaling pathways, causing many biochemical reactions in cells. PI3-K also has serine / threonineproteinkinase activity, which can regulate its own phosphoinositide kinase activity; The activation of PI3-K has a great relationship with cell growth, differentiation and cell survival. Deregulation of PI3K-Akt signaling pathway is a stimulating signal for the occurrence of various tumors, and abnormal expression of any kinase in the signaling pathway may induce tumorigenesis. [0003] With the research on PI3-K signal transduction and t...
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