59826-47-0Relevant academic research and scientific papers
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.
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.
Solvent-free synthesis, spectral correlations and antimicrobial activities of some aryl e 2-propen-1-ones
Sathiyamoorthi,Mala,Sakthinathan,Kamalakkannan,Suresh,Vanangamudi,Thirunarayanan
, p. 245 - 256 (2013/11/06)
Totally 38 aryl E 2-propen-1-ones including nine substituted styryl 4-iodophenyl ketones have been synthesised using solvent-free SiO 2-H3PO4 catalyzed Aldol condensation between respective methyl ketones and substituted benzaldehydes under microwave irradiation. The yields of the ketones are more than 80%. The synthesised chalcones were characterized by their analytical, physical and spectroscopic data. The spectral frequencies of synthesised substituted styryl 4-iodophenyl ketones have been correlated with Hammett substituent constants, F and R parameters using single and multi-linear regression analysis. The antimicrobial activities of 4-iodophenyl chalcones have been studied using Bauer-Kirby method.
Preheated fly-ash catalyzed aldol condensation: Efficient synthesis of chalcones and antimicrobial activities of some 3-thienyl chalcones
Arulkumaran, Ranganathan,Vijayakumar, Sambandhamoorthy,Sakthinathan, S. Pazhanivel,Kamalakkannan, Dakshnamoorthy,Ranganathan, Kaliyaperumal,Suresh, Ramamoorthy,Sundararajan, Rajasekaran,Vanangamudi, Ganesan,Thirunarayanan, Ganesamoorthy
, p. 1684 - 1690 (2013/09/24)
In the present study we have prepared a series of some chalcones using solvent - free Aldol - condensation by microwave irradiation. The yields of the ketones are more than 60%. The synthesised chalcones were characterized by their analytical, physical and spectral data. The antimicrobial activities of substituted styryl 3-thienyl ketones have been studied using Bauer-Kirby method.
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
Fly-ash:H2SO4 catalyzed solvent free efficient synthesis of some aryl chalcones under microwave irradiation
Thirunarayanan,Mayavel,Thirumurthy
experimental part, p. 18 - 22 (2012/05/05)
Some 2E aryl chalcones have been synthesized using greener catalyst Fly-ash:H2SO4 assisted solvent free environmentally benign Crossed-Aldol reaction. The yields of chalcones are more than 90%. The synthesized chalcones are characterized by their physical constants and spectral data.
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
Synthesis, molecular modeling and biological evaluation of chalcone thiosemicarbazide derivatives as novel anticancer agents
Zhang, Hong-Jia,Qian, Yong,Zhu, Di-Di,Yang, Xu-Guang,Zhu, Hai-Liang
experimental part, p. 4702 - 4708 (2011/10/31)
A series of novel chalcone thiosemicarbazide derivatives (4a-4x) have been designed, synthesized, structurally determined, and their biological activities were also evaluated as potential EGFR kinase inhibitors. All the synthesized compounds are first reported. Among the compounds, compound 4r showed the most potent biological activity (IC50 = 0.78 ± 0.05 μM for HepG2 and IC50 = 0.35 μM for EGFR), which is comparable to the positive controls. Docking simulation was also performed to position compound 4r into the EGFR active site to determine the probable binding model. Antiproliferative assay results demonstrated that some of these compounds possessed good antiproliferative activity against HepG2. Compound 4r with potent inhibitory activity in tumor growth inhibition may be a potential anticancer agent.
Synthesis and insect antifeedant activities of some substituted styryl 3,4-dichlorophenyl ketones
Thirunarayanan,Surya,Srinivasan,Vanangamudi,Sathiyendiran
experimental part, p. 152 - 156 (2010/02/16)
Sixteen substituted styryl 3,4-dichlorophenyl ketones [(2E)-1-(3,4-dichlorophenyl)-3-phenyl-2-propen-1-ones] were synthesized using eco-friendly benign stereoselective crossed-aldol reaction. They are characterized by their analytical, infrared, NMR and m
Synthesis, molecular modeling and biological evaluation of dithiocarbamates as novel antitubulin agents
Qian, Yong,Ma, Gao-Yuan,Yang, Ying,Cheng, Kui,Zheng, Qing-Zhong,Mao, Wen-Jun,Shi, Lei,Zhao, Jing,Zhu, Hai-Liang
experimental part, p. 4310 - 4316 (2010/09/12)
A series of novel dithiocarbamate compounds with the chalcone scaffold have been designed and synthesized, and their biological activities were also evaluated as potential antiproliferation and antitubulin polymerization inhibitors. Compound 2n showed the most potent biological activity in vitro, which inhibited the growth of MCF-7 cells with IC50 of 0.04 ± 0.01 μM and the polymerization of tubulin with IC50 of 6.8 ± 0.6 μM. To understand the tubulin-inhibitor interaction and the selectivity of the most active compound towards tubulin, molecular modeling studies were performed to dock compound 2n into the colchicine binding site, which suggested probable inhibition mechanism.
