76973-45-0Relevant academic research and scientific papers
Biosynthesis of ZrO2 for ZrO2@Ag-S-CH2COOH as the retrievable catalyst for the one-pot green synthesis of pyrazoline derivatives and their anticancer evaluation
Gurav, Rutikesh Pandit,Nalawade, Rohit Dattatray,Sawant, Shivaji Dnyandeo,Satyanarayan, Nayak Devappa,Sankpal, Sandeep Ashok,Hangirgekar, Shankar Poshatti
, (2022/04/03)
In the present work, Ficus benghalensis leaf extract was used for the synthesis of ZrO2 nanoparticles. Further, ZrO2@Ag-S-CH2-COOH was synthesized using biosynthesized ZrO2, and its catalytic potential was examined in the synthesis of pyrazoline from reaction of chalcone and hydrazine hydrate at room temperature. The structural conformation of ZrO2@Ag-S-CH2-COOH has been done using FT-IR, SEM, EDX, XRD, TGA-TDA, XPS, and DLS techniques, high turnover number (TON), and high turnover frequency. The ZrO2@Ag-S-CH2-COOH demonstrated outstanding catalytic activity for the synthesis of pyrazolines. The structures of the pyrazoline derivatives were confirmed by FT-IR, 1H and 13C NMR, and mass spectrometry techniques. Synthesized pyrazoline were tested for anticancer activity against human lung cancer cell line A549 study and confirmed by molecular docking investigations.
Dihydropyrazole sulfonamides compound and preparation method and application thereof (by machine translation)
-
, (2020/07/28)
The invention discloses a dihydropyrazole sulfonamides compound and a preparation method and application thereof, wherein the dihydropyrazole sulfonamide compound has the following general formula. Wherein R is hydrogen or R1 Selected from OCH
Discovery and Pharmacophore Studies of Novel Pyrazole-Based Anti-Melanoma Agents
Li, Qing-Shan,Lü, Xian-Hai,Yang, Yang,Ruan, Ban-Feng,Yao, Ri-Sheng,Liao, Chen-Zhong
, p. 116 - 132 (2015/10/19)
Due to the rising incidence and lack of effective treatments, malignant melanoma is the most dangerous form of skin cancer, so that new treatment strategies are urgently needed. Several recent developments indicate that the V600E mutant BRAF (BRAFV60
Design, modification and 3D QSAR studies of novel 2,3-dihydrobenzo[b][1,4] dioxin-containing 4,5-dihydro-1H-pyrazole derivatives as inhibitors of B-Raf kinase
Yang, Yu-Shun,Li, Qing-Shan,Sun, Shuai,Zhang, Yan-Bin,Wang, Xiao-Liang,Zhang, Fei,Tang, Jian-Feng,Zhu, Hai-Liang
, p. 6048 - 6058 (2012/11/07)
Two series of novel 2,3-dihydrobenzo[b][1,4]dioxin-containing 4,5-dihydro-1H-pyrazole derivatives C1-C15 and D1-D15 have been synthesized and evaluated for their B-Raf inhibitory and anti-proliferation activities. Compound C14 ((3-(4-bromophenyl)-5-(2-fluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl)(2,3- dihydrobenzo[b][1,4]dioxin-6-yl)methanone) showed the most potent biological activity against B-RafV600E (IC50 = 0.11 μM) and WM266.4 human melanoma cell line (GI50 = 0.58 μM), being comparable with the positive control Erlotinib and more potent than our previous best compound, while D10 ((2,3-dihydrobenzo[b][1,4]dioxin-2-yl)(5-(3- fluorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)methanone) performed the best in the D series (IC50 = 1.70 μM; GI50 = 1.45 μM). The docking simulation was performed to analyze the probable binding models and poses and the QSAR model was built for reasonable design of B-Raf inhibitors in future. The introduction of 2,3-dihydrobenzo[b][1,4]dioxin structure reinforced the combination of our compounds and the receptor, resulting in progress of bioactivity.
Identification of novel 3,5-diarylpyrazoline derivatives containing salicylamide moiety as potential anti-melanoma agents
Li, Qing-Shan,Zhang, Yan-Bin,Dong, Jing-Jun,Zhou, Wen-Ping,Yang, Yang,Zhu, Hai-Liang,Lv, Xian-Hai
, p. 6596 - 6601,6 (2012/12/12)
There is an accumulating body of experimental evidences validating oncogenic BRAFV600E as a therapeutic target and offering opportunities for anti-melanoma drug development. Encouraged by the positive results of pyrazole derivatives as BRAFsup
Synthesis, biological evaluation and 3D-QSAR studies of novel 4,5-dihydro-1H-pyrazole niacinamide derivatives as BRAF inhibitors
Li, Cui-Yun,Li, Qing-Shan,Yan, Li,Sun, Xiao-Guang,Wei, Ran,Gong, Hai-Bin,Zhu, Hai-Liang
, p. 3746 - 3755 (2012/08/28)
A series of novel 4,5-dihydropyrazole derivatives containing niacinamide moiety as potential V600E mutant BRAF kinase (BRAFV600E) inhibitors were designed and synthesized. Results of the bioassays against BRAF V600E and WM266.4 human
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.
