72098-52-3Relevant academic research and scientific papers
Mechanistic investigations on substituted benzene sulphonamides as apoptosis inducing anticancer agents
Mettu, Akhila,Naikal James Prameela, Subhashini,Talla, Venu,Thumma, Soujanya
, (2020/01/28)
In an approach to develop potent cytotoxic compounds with targeted action, a systematic methodology was employed to design and initially synthesize parent compounds A1, A8, A13 and A14 followed by synthesis of further analogs of A1 (A2-A7) and A8 (A9-A12)
Design, synthesis, and biological evaluation of novel thienopyrimidine derivatives as PI3Kα inhibitors
Yu, Lide,Wang, Qinqin,Wang, Caolin,Zhang, Binliang,Yang, Zunhua,Fang, Yuanying,Zhu, Wufu,Zheng, Pengwu
, (2019/10/02)
Three series of novel thienopyrimidine derivatives 9a-l, 15a-l, and 18a-h were designed and synthesized, and their IC50 values against four cancer cell lines HepG-2, A549, PC-3, and MCF-7 were evaluated. Most compounds show moderate cytotoxicity against the tested cancer cell lines. The most promising compound 9a showed moderate activity with IC50 values of 12.32 ± 0.96, 11.30 ± 1.19, 14.69 ± 1.32, and 9.80 ± 0.93 μM, respectively. The inhibitory activities of compounds 9a and 15a against PI3Kα and mTOR kinase were further evaluated. Compound 9a exhibited PI3Kα kinase inhibitory activity with IC50 of 9.47 ± 0.63 μM. In addition, docking studies of compounds 9a and 15a were also investigated.
Synthesis and bioevaluation of thienopyrimidines bearing a pyrazoline unit as selective PI3Kα inhibitors
Lai, Luogen,Wang, Qinqin,Zhang, Binliang,Xiao, Zhen,Yang, Zunhua,Yang, Qi,Luo, Zixin,Zhu, Wufu,Xu, Shan
, p. 29579 - 29589 (2019/10/01)
A series of thienopyrimidines containing a pyrazoline unit (4a-d, 7a-d and 13a-l) were designed and synthesized. The target compounds were evaluated for antiproliferative activity against A549, HepG2 and MCF-7 cancer cell lines. Among the twenty target compounds, most of them exhibited excellent antiproliferative activity against one or several cancer cell lines. Compound 13f showed the best activity against A549, MCF-7 and HepG2 cancer cell lines, with IC50 values of 2.84 ± 0.09 μM, 2.88 ± 0.43 μM and 2.08 ± 0.36 μM, respectively. Four selected compounds (13c, 13f, 13g and 13h) were further evaluated for their inhibitory activity against the PI3Kα/mTOR protein kinase. Moreover, time-dependent and dose-dependent experiments, AO fluorescence staining, Annexin V-FITC/PI staining and docking studies were carried out in this study. The results indicated that compound 13f may be a potential selective PI3Kα inhibitor.
Synthesis and antifungal activity of chalcone derivatives
Zheng, Yuanyuan,Wang, Xuesong,Gao, Sumei,Ma, Min,Ren, Guiming,Liu, Huabing,Chen, Xiaohong
, p. 1804 - 1810 (2015/03/04)
In the present study, using chalcone as a lead compound, a series of its derivatives (compounds 1-30) were designed and synthesised. Their activity of anti-pathogenic fungi of plants has been evaluated. It is found that these compounds have good antifunga
Solvent-free synthesis of some1-acetyl pyrazoles
Thirunarayanan, Ganesamoorthy,Sekar, Krishnamoorthy Guna
supporting information, p. 599 - 605 (2013/11/06)
Some N-acetyl pyrazoles including 1-(3-(3,4-dichlorophenyl)-5-(substituted phenyl)-4,5-dihydro-1H-pyrazole-1-yl) ethanones have been synthesised by solvent free cyclization cum acetylation of chalcones like substituted styryl 3,4-dichlorophenyl
Synthesis, biological evaluation and molecular modeling of dihydro-pyrazolyl-thiazolinone derivatives as potential COX-2 inhibitors
Qiu, Ke-Ming,Yan, Ru,Xing, Man,Wang, Hai-Hong,Cui, Hong-En,Gong, Hai-Bin,Zhu, Hai-Liang
, p. 6648 - 6654 (2013/01/15)
A series of dihydro-pyrazolyl-thiazolinone derivatives (5a-5t) have been synthesized and their biological activities were also evaluated as potential cyclooxygenase-2 (COX-2) inhibitors. Among these compounds, compound 2-(3-(3,4-dimethylphenyl)-5-phenyl-4
