925675-85-0Relevant articles and documents
Pyrazolo[1,5-a]pyrimidine compounds and application thereof
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Paragraph 0047; 0048; 0049, (2018/09/20)
The invention discloses pyrazolo[1,5-a]pyrimidine compounds and application thereof, and belongs to the field of medicines. Some of the pyrazolo[1,5-a]pyrimidine compounds has the inhibitory activityof 40% or more against CDK2, so that the compounds have good inhibitory activity against CDK2 and can be used as a CDK2 inhibitor. The compounds have stronger inhibitory activity against CDK2 and haveimportant guiding significance for the development of drugs suitable for use as CDK2 inhibitors.
Pyrazolo [1, 5 - a] pyrimidine nitrogen mustard derivative and its preparation method and tumor therapeutic use
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Paragraph 0132; 0133; 0134; 0135; 0136, (2017/08/02)
The invention relates to pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives or medical salts thereof, as well as application of the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives or the medical salts thereof. The pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives and the medical salts thereof have the structure shown as the formula I. Pharmacological experiments show that the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives and the medical salts thereof have inhibiting effects on the proliferation of various tumor cells. Moreover, the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives are small in toxicity, have the advantages of selectivity on tumor cells, and are dual-functional anti-tumor drugs. Meanwhile, the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives are easy to synthesize, and the overall yields are high. All the advantages show that the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives have great potential of being anti-tumor drugs.
18F-labeled pyrazolo[1,5-a]pyrimidine derivatives: Synthesis from 2,4-dinitrobenzamide and tosylate precursors and comparative biological evaluation for tumor imaging with positron emission tomography
Xu, Jingli,Liu, Hang,Li, Guixia,He, Yong,Ding, Rui,Wang, Xiao,Feng, Man,Zhang, Shuting,Chen, Yurong,Li, Shilei,Zhao, Mingxia,Li, Yingruo,Qi, Chuanmin,Dang, Yonghong
scheme or table, p. 3774 - 3793 (2012/07/28)
We previously reported 18F-labeled pyrazolo[1,5-a]pyrimidine derivatives: 7-(2-[18F]fluoroethylamino)-5-methylpyrazolo[1,5-a] pyrimidine-3-carbonitrile ([18F]1) and N-(2-(3-cyano-5- methylpyrazolo[1,5-a]pyrimidin-7-ylamino)ethyl)-2-[18F]fluoro-4- nitrobenzamide ([18F]2). Preliminary biodistribution experiments of both compounds showed s slow clearance rate from excretory tissues which warranted further investigation for tumor imaging with PET. Here we modified [18F]1 and [18F]2 by introducing polar groups such as ester, hydroxyl and carboxyl and developed three additional 18F-18 labeled pyrazolo[1,5-a] pyrimidine derivatives: (3-Cyano-7-(2-[ 18F]fluoroethylamino)pyrazolo[1,5-a]-pyrimidin-5- yl)methyl acetate ([18F]3), 7-(2-[18F]fluoroethylamino)-5-(hydroxymethyl) pyrazolo[1,5-a]- pyrimidine-3-carbonitrile ([18F]4) and (S)-6-(3-cyano-5-methylpyrazolo[1,5-a]pyrimidin-7- ylamino)-2-(2-[ 18F]fluoro-4-nitrobenzamido)hexanoic acid ([18F]5). The radiolabeled probes were synthesized by nucleophilic substitution of the corresponding tosylate and nitro precursors with 18F-fluoride. In Vitro studies showed higher uptake of [18F]3 and [18F]4 than that of [18F]5 by S180 tumor cells. In Vivo biodistribution studies in mice bearing S180 tumors showed that the uptake of both [ 18F]3 and [18F]4 in tumors displayed an increasing trend while the uptake of [18F]5 in tumor decreased through the course of the 120 min study. This significant difference in tumor uptake was also found between [18F]1 and [18F]2. Thus, we compared the biological behavior of the five tracers and reported the tumor uptake kinetic differences between 2-[18F]fluoroethylamino- and 2-[ 18F]fluoro-4-nitro- benzamidopyrazolo[1,5-a] pyrimidine derivatives.
Synthesis and biological evaluation of pyrazolo[1,5-a]-pyrimidine- containing 99mTc nitrido radiopharmaceuticals as imaging agents for tumors
Ding, Rui,He, Yong,Xu, Jingli,Liu, Hang,Wang, Xiao,Feng, Man,Qi, Chuanmin,Zhang, Junbo
scheme or table, p. 8723 - 8733 (2011/02/28)
The compound 5-((2-aminoethylamino)methyl)-7-(4-bromoanilino)-3- cyanopyrazolo[ 1,5-a]pyrimidine (ABCPP) was synthesized and conjugated with N-mercaptoacetylglycine (MAG), N-mercaptoacetylphenylalanine (MAF) and N-mercaptoacetylvaline (MAA), respectively. These three compounds were labeled successfully with [99mTcN]2+ intermediate in high radiochemical purities. Biodistribution in tumor-bearing mice demonstrated that the three new complexes showed tumor accumulation, high tumor-tomuscle (T/M) ratios and fast clearance from blood and muscle. Among them, the 99mTcNMAG-ABCPP showed the most favorable characteristics, with tumor/blood and tumor/muscle ratios reaching 1.51 and 2.97 at 30 min post-injection, 1.84 and 2.49 at 60 min post-injection, suggesting it could be further studied as potential tumor imaging agent for single photon emission computed tomography (SPECT).
Synthesis and anti-tumor activities of novel pyrazolo[1,5-a]pyrimidines
Li, Juan,Zhao, Yan Fang,Zhao, Xiang Lin,Yuan, Xiao Ye,Gong, Ping
, p. 593 - 597 (2007/10/03)
A series of novel pyrazolo[1,5-a]pyrimidines were designed and synthesized in order to find novel potent anti-tumor compounds. The structures of all the compounds were confirmed by IR, 1H-NMR, elemental analysis, and MS. Their anti-tumor activities against cancer cell lines were tested by the MTT method in vitro. Compound 19 displayed potent anti-tumor activity.
