57073-26-4Relevant academic research and scientific papers
Synthesis, characterization, molecular docking and in vitro anticancer activity of 3-(4-methoxyphenyl)-5-substituted phenyl-2-pyrazoline-1-carbothioamide
Sahu, Benupani,Rajapandi,Maji, Avik,Paul, Abhik,Singha, Tanushree,Maity, Tapan Kumar
, p. 1648 - 1658 (2021/06/26)
In the present study, eight numbers of new 3-(4-methoxy phenyl)-5-substituted phenyl-2-pyrazoline-1-carbothioamide (5a-h) have been synthesized from 1-(4-methoxy phenyl)-3-(substituted phenyl)-prop-2-en-1-one (3a-h) and structurally characterized by using FT-IR,1H NMR,13C NMR, Mass and Elemental analysis. The synthesized molecules were biologically eval-uated for their in vitro anticancer activity against human breast adenocar-cinoma (MCF-7), liver cancer (Hep-G2) and leukaemia cancer (K-562) cell line using Sulforhodamine B (SRB) bioassay technique. From the all synthesized compounds 5a, 5c, 5d, and 5e exhibited potent anticancer activity (GI50= 50=44.5μg/ml) and Adriamycin (ADR) (GI50= 10μg/ml) on MCF-7 cell lines. Besides this, all the synthesized compounds have exhibited moderate activity against human liver cancer (Hep-G2) and leukaemia cancer (K-562) cell lines. In addition, molecular docking studies were also explored in order to study the probable binding specificity into the active site of Epidermal Growth Factor Receptor tyrosine kinase (EGFR) (PDB ID: 1M17) using Molegro Virtual Docker Evaluation 2013 6.0.1 (MVD). Based on the molecular docking result, it was found that compound 5a exhibited the best interaction with the above target (i.e., EGFR) by interacting with specific amino acid residues such as: Thr 766, Gin 767, Thr 830, Cys 575, Ala 719 and Met 769.
Synthesis of polysubstituted pyridines under combined microwave and ultrasound irradiation: K2CO3-promoted tandem addition/cyclization/hydrogen shift process
Feng, Huangdi,Li, Yuan,Van Der Eycken, Erik V.,Peng, Yanqing,Song, Gonghua
supporting information; experimental part, p. 1160 - 1162 (2012/03/26)
A convenient and efficient K2CO3-promoted tandem reaction of chalcone, malononitrile, and methanol for the synthesis of highly functionalized pyridines has been developed. This multi-component reaction employing the weak nucleophilic agent methanol proceeded smoothly under combined microwave and ultrasound irradiation (CMUI). The reaction mechanism was proposed to consist of a Michael addition, a methoxylation of CN bond, a cyclization to a 1,4-dihydropyridine and an intermolecular hydrogen shift between 1,4-dihydropyridine and initial chalcone.
Synthesis and protein tyrosine phosphatase 1B-Inhibitory activity of chalcones
Zhao, Fei,Zhao, Qing-Jie,Zhang, Da-Zhi,Jin, Yong-Sheng,Zhang, Wei
experimental part, p. 5339 - 5342 (2012/06/30)
Protein tyrosine phosphatase 1B (PTP1B) is an effective target for the treatment of type 2 diabetes and obesity. So far less work has been conducted in the structure-activity relationship of the PTP1B inhibitory activity of chalcones. In this work, a libr
Synthesis and biological activity of 3-aryl-5-(3′ -bromo/chlorophenyl)isoxazoles
Popat,Nimavat,Kachhadia,Joshi
, p. 707 - 708 (2007/10/03)
3-Aryl-5-(3′-bromo/chlorophenyl)isoxazole derivatives (3a-j, 4a-j) have been prepared by condensing 1-aryl-3-(3′-bromo/ chlorophenyl)-2-propen-1-ones (1a-j, 2a-j) with hydroxylamine hydrochloride. Compounds 1a-j, 2a-j have been synthesized by the reaction
Kinetic Study of the Homolytic Brominolysis of 1,2-Diarylcyclopropanes
Applequist, Douglas E.,Gdanski, Rick D.
, p. 2502 - 2510 (2007/10/02)
The rate constants for the photolytic brominolysis of 22 trans-1,2-diarylcyclopropanes in carbon disulfide relative to an internal standard, p-chlorotoluene, have been determined.The products of the brominolysis are 1,3-dibromo-1,3-diarylpropanes.The rate constants range over 5 orders of magnitude, being enhanced by electrondonating substituents on one or both benzene rings.The quantitative size of the substituent effect (ρ) at either involved carbon center is a function of the substituent at the other center.This fact suggests a continuum of transition-state structures with varying degrees of bond breaking and charge separation.
