41167-58-2Relevant academic research and scientific papers
Synthesis of Functionalized Cyclobutenes and Spirocycles via Asymmetric P(III)/P(V) Redox Catalysis
Lorton, Charlotte,Roblin, Antoine,Retailleau, Pascal,Voituriez, Arnaud
supporting information, p. 4805 - 4810 (2021/09/08)
An enantioselective phosphine-catalyzed transformation has been developed for the synthesis of chiral cyclobutene triesters and fluorinated spirocyclic compounds. The strategy involved a P(III)/P(V) redox cycling process, via in situ reduction of phosphin
Design, syntheses and antitumor activities evaluation of 1,5-diaryl substituted pyrazole secnidazole ester derivatives
Teng, Qing-Hu,Sun, Gui-Xia,Luo, Shu-Ying,Wang, Kai,Liang, Fu-Pei
supporting information, p. 1656 - 1664 (2021/05/29)
According to the drug hybridization principle, a series of novel 1,5-diaryl substituted pyrazole secnidazole ester derivatives (6aa–6gc) have been synthesized by the combinations of various 1,5-diarylpyrazole-3-carboxylic acids with secnidazole. The in vi
Pyrrole and pyrazole compound of preparation and use as medicaments (by machine translation)
-
Paragraph 0071; 0072; 0073; 0074, (2018/03/26)
The invention relates to the field of medical technology, this invention has offered a kind of sulfonamide and nitrogen mixed uncle butane pyrrole and pyrazole compound, including optical isomers, racemic modification, and any combination of the trans isomer or a pharmaceutically acceptable salt thereof, having a structure of formula (I); the invention also provides the preparation method of the compound and its application, in particular in the preparation of anti-tumor drug application. (by machine translation)
Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition
Ren, Shen-Zhen,Wang, Zhong-Chang,Zhu, Xiao-Hua,Zhu, Dan,Li, Zhang,Shen, Fa-Qian,Duan, Yong-Tao,Cao, Han,Zhao, Jing,Zhu, Hai-Liang
, p. 4264 - 4275 (2018/07/21)
The overexpress of COX-2 was clearly associated with carcinogenesis and COX-2 as a possible target has long been exploited for cancer therapy. In this work, we described the design and synthesis of a series of diarylpyrazole derivatives integrating with c
Diacylhydrazines derivative containing indole skeleton as well as preparation method and application thereof
-
Paragraph 0045; 0048, (2018/10/11)
The invention discloses a diacylhydrazines derivative containing an indole skeleton as well as a preparation method and application thereof. A structure of the diacylhydrazines derivative containing the indole skeleton disclosed by the invention is shown in a formula: the formula (1) is shown in the description, wherein R1 is selected from -H and -F; R2 is selected from -H and -Br; R3 is selectedfrom -H, -Cl and -I; R4 is selected from -CH3, -Cl, -H, -F and -CF3. A synthetic method of the diacylhydrazines derivative has the advantages of simple process, less steps, lower cost, high efficiencyand convenience and has good universality, and moreover, the diacylhydrazines derivative can be produced in batch.
Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX
Shen, Fa-Qian,Wang, Zhong-Chang,Wu, Song-Yu,Ren, Shen-Zhen,Man, Ruo-Jun,Wang, Bao-Zhong,Zhu, Hai-Liang
supporting information, p. 3653 - 3660 (2017/07/27)
In our previous study, we designed a series of pyrazole derivatives as novel COX-2 inhibitors. In order to obtain novel dual inhibitors of COX-2 and 5-LOX, herein we designed and synthesized 20 compounds by hybridizing pyrazole with substituted coumarin w
Design, synthesis and structure–activity relationship of 4,5-dihydropyrrolo[3,4-c]pyrazol-6(1H)-ones as potent p53-MDM2 inhibitors
Zhou, Wei-Huang,Xu, Xi-Guo,Li, Jin,Min, Xiao,Yao, Jian-Zhong,Dong, Guo-Qiang,Zhuang, Chun-Lin,Miao, Zhen-Yuan,Zhang, Wan-Nian
supporting information, p. 422 - 425 (2017/01/28)
In the past decade, the p53-MDM2 protein–protein interaction by small molecules has been confirmed as a successful strategy for cancer therapy. In our previous work, pyrrolo[3,4-c]pyrazol-6(1H)-ones were found to be potent p53-MDM2 inhibitors. Further optimization and structure–activity relationship studies were described in the present work. The result revealed that benzyl group on position N1 of imidazole and bromine on C4-phenyl of pyrrolidone showed higher inhibitory activities. In vitro antiproliferative assay demonstrated the potent p53-MDM2 inhibitor 5c with 4-fold selectivity for U2 OS and Saos-2 cells. These data indicated that 4,5-dihydropyrrolo[3,4-c]pyrazol-6(1H)-one moiety is a valuable scaffold for further development of p53-MDM2 inhibitors.
Gyrrolone and pyrromonazole compound and its use as medicine
-
Paragraph 0068-0071, (2016/11/14)
The present invention belongs to the technical field of medicine. Provided in the present invention is pyrrolidone compounds, including optical isomers, racemates, cis and trans isomers and any combination thereof or pharmaceutically acceptable salts thereof, having a structure as shown in formula (I). The compounds of the present invention can be used as a small molecule inhibitor for p53-MDM2/X protein interactions. The compounds of the present invention can be used to prepare antineoplastic or anti-inflammatory drugs.
Design, synthesis and evaluation of benzenesulfonamide-substituted 1,5-diarylpyrazoles containing phenylacetohydrazide derivatives as COX-1/COX-2 agents against solid tumors
Lu, Xiao-Yuan,Wang, Zhong-Chang,Wei, Ting,Yan, Xiao-Qiang,Wang, Peng-Fei,Zhu, Hai-Liang
, p. 22917 - 22935 (2016/03/15)
Novel benzenesulfonamide-substituted 1,5-diarylpyrazoles containing phenylacetohydrazide derivatives have been designed, synthesized and evaluated for their biological activities as selective COX-2 inhibitors with anticancer potential. In vitro the bioass
Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis
Lu, Xiao-Yuan,Wang, Zhong-Chang,Ren, Shen-Zhen,Shen, Fa-Qian,Man, Ruo-Jun,Zhu, Hai-Liang
supporting information, p. 3491 - 3498 (2016/07/21)
Cyclooxygenase-2 is frequently overexpression in malignant tumors and the product PGE2promotes cancer cell progression and metastasis. We designed novel series of coumarin sulfonamides derivatives to improve biological activities of COX-2 inhib
