20532-69-8Relevant academic research and scientific papers
Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists
Chu, Bizhu,Jiang, Yuyang,Li, Qinyuan,Liu, Zijian,Luo, Jingyi,Shi, Zhichao,Xin, Qilei,Ye, Lizhen,Zhan, Feng,Zhang, Xun,Zhu, Qingyun
, (2021/09/20)
Chemokine receptor 2 (CXCR2) is the receptor of glutamic acid–leucine–arginine sequence-contained chemokines CXCs (ELR+ CXCs). In recent years, CXCR2-target treatment strategy has come a long way in cancer therapy. CXCR2 antagonists could block
Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors
Hu, Hao,Chen, Fei,Dong, Yuhong,Li, Ming,Xu, Sicong,Qin, Mingze,Gong, Ping
, (2020/07/31)
Clinically, a single agent that simultaneously inhibits multiple targets has been widely used in cancer treatment to overcome complicated dose design and anti-cancer resistance. Inspired by the synergistic effects between c-Met and HDAC in tumor developme
Design, synthesis and biological evaluation of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2H)-one fragment
Duan, Yongli,Tang, Qidong,Xiong, Hehua,Zhang, Han,Zhang, Jianqing,Zhang, Qian,Zheng, Pengwu
, (2020/03/23)
A series of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2H)-one fragment were designed, synthesized, and evaluated for their biological activity. Most compounds showed effective inhibitory activity against cancer cell lines of A
Discovery of novel 7-azaindole derivatives bearing dihydropyridazine moiety as c-Met kinase inhibitors
Tang, Qidong,Wang, Linxiao,Duan, Yongli,Wang, Wenhui,Huang, Shunmin,Zhi, Jia,Jia, Shuang,Zhu, Wufu,Wang, Ping,Luo, Rong,Zheng, Pengwu
, p. 97 - 106 (2017/04/07)
A series of 7-azaindole derivatives bearing the dihydropyridazine scaffold were synthesized and evaluated for their c-Met kinase inhibitory, and antiproliferative activity against 4 cancer cell lines (HT29, A549, H460, U87MG) were evaluated in?vitro. Most compounds showed moderate to excellent potency. Compared to foretinib, the most promising analog 34 (c-Met IC50: 1.06?nM, a multitarget tyrosine kinase inhibitor) showed a 6.4-, 7.8-, and 3.2-fold increase in activity against HT29, A549, and H460?cell lines, respectively. Structure activity relationship studies indicated that mono-EWGs (such as R2?=?F) at 4-position of moiety D was a key factor in improving the antitumor activity.
Design, synthesis and structure-activity relationships of novel 4-phenoxyquinoline derivatives containing pyridazinone moiety as potential antitumor agents
Zhou, Shunguang,Liao, Huimin,He, Chao,Dou, Yanan,Jiang, Mingyan,Ren, Lixiang,Zhao, Yanfang,Gong, Ping
, p. 581 - 593 (2014/07/21)
A series of novel 4-phenoxyquinoline derivatives containing pyridazinone moiety were synthesized and evaluated for their in vitro cytotoxic activity against five cancer cell lines (HT-29, H460, A549, MKN-45, and U87MG). Most of the compounds exhibited moderate-to-significant cytotoxicity and high selectivity against one or more cell lines. Compounds 15a, 20a, 15b, 15c, 20d, and 16e were further examined for their inhibitory activity against c-Met kinase. The most promising compound 15a (c-Met half-maximal inhibitory concentration [IC50] = 2.15 nM) showed remarkable cytotoxicity against HT-29, H460, and A549 cell lines with IC50 values of 0.10 μM, 0.13 μM, and 0.05 μM, respectively, and thus it was 1.5- to 2.3-fold more potent than foretinib. Their preliminary structure-activity relationships (SARs) studies indicate that electron-withdrawing groups on the terminal phenyl rings are beneficial for improving the antitumor activity.
Synthesis and antimicrobial activity of pyrazolinones and pyrazoles having benzothiazole moiety
Amir, Mohd.,Javed, Sadique A.,Hassan, Mohd. Zaheen
experimental part, p. 1261 - 1270 (2012/07/31)
A new class of 4-arylhydrazono-1-benzothiazolyl-3-methylpyrazolin-5-ones (3a-j) and 4-arylazo-1-benzothiazolyl-3,5-dimethylpyrazoles (4a-j) were designed as pharmacophore hybrids between pyrazolinone/pyrazole and benzothiazole moiety. The target molecules were efficiently synthesized by the cyclization of various oxobutyrates/pentane-2,4-dione derivatives with 6-chloro-2- hydrazinobenzothiazole in the presence of glacial acetic acid. The compounds were evaluated for their in vitro antimicrobial activity. Preliminary study of the structure-activity relationship revealed that electron-withdrawing groups in phenyl ring had a promising effect on the antimicrobial activity. Also, correlation study has been used to establish the relationships between the antibacterial activity and physicochemical parameter clogP. Springer Science+Business Media, LLC 2011.
Synthesis, characterization and antibacterial screening of new pyrazole and pyrazoline-5-one derivatives
Nagaraju,Srinivasulu,Doraswamy,Venkata Ramana
experimental part, p. 293 - 298 (2012/03/11)
A series of N′-(p-toluene sulphonyl)-3-methyl-4-(substituted arylhydrazono)-2-pyrazoline-5-ones and N′-(2-hydroxybenzoyl)-3,5-dimethyl- 4-(substituted arylazo)pyrazoles have been synthesized and characterized by chemical analysis, IR and 1H NMR spectral data. The compounds have been screened for antibacterial activity against Staphylococcus aureus and Escherichia coli.
Synthesis of N′-(2-hydroxybenzoyl)-3-methyl-4-(substituted-phenylhydrazono)-2- pyrazolin-5-ones
Venkata Ramana,Ravindranath
, p. 112 - 113 (2007/10/03)
N′-(2-Hydroxybenzoyl)-3-methyl-4-(substituted-phenylhydrazono)-2- pyrazolin-5-ones have been synthesised by the reaction of 2-(substituted-phenylhydrazono)-ethyl-2,3-dioxobutyrate with salicylic acid hydrazine.
On the Polarographic Reduction Mechanism of Some Heterocyclic Compounds
Malik, Wahid U.,Jain, Rajeev
, p. 191 - 194 (2007/10/02)
For evaluating the mechanistic steps, position at d.m.e. and assigning inner or outer sphere path of electrode processes of a number of pyrazole derivatives, thiazoles and their precursors experiments were carried out in the absence and presence of surfactants.All the compounds gave diffusion-controlled, irreversible waves over the entire pH range (2.0-11.0) studied.In presence of surfactants also, diffusion-controlled but more irreversible waves were obtained.In absence and presence of surfactant (CTAB) values of Kapp and αapp for all these compounds were calculated and have been taken as a proof of inner sphere or outer sphere path of the electrode reaction.Results have been explained on the basis of formation of phenylazo-functionalised surfactant as an intermediate species.
