75745-48-1Relevant academic research and scientific papers
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
One-pot synthesis of 3,5-diphenyl-1h-pyrazoles from chalcones and hydrazine under mechanochemical ball milling
Zhang, Ze,Tan, Ya-Jun,Wang, Chun-Shan,Wu, Hao-Hao
, p. 103 - 112 (2014/02/14)
A highly efficient and environmentally friendly method has been developed for facile synthesis of 3,5-diphenyl-1H-pyrazoles under mechanochemical ball-milling conditions. The advantages of short reaction time, high efficiency, no separation of in situ generated intermediate, using cheap sodium persulfate as the oxidant, together with very simple work-up procedure, make this one-pot and solvent-free protocol a green and powerful alternative to traditional methods for the synthesis of these kinds of compounds.
Exploration of the SAR of anti-invasive chalcones: Synthesis and biological evaluation of conformationally restricted analogues
Roman, Bart I.,Ryck, Tine De,Dierickx, Laura,Vanhoecke, Barbara W.A.,Katritzky, Alan R.,Bracke, Marc,Stevens, Christian V.
experimental part, p. 4812 - 4819 (2012/09/08)
In order to get a clearer view on the active geometry of anti-invasive chalcones, we have prepared a number of isoxazoles and related substances as conformationally restrained mimics of 1,3-diarylpropenones, and also of (Z)-stilbenes. In vitro anti-invasi
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
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 of new 4-thiazolidinone-, pyrazoline-, and isatin-based conjugates with promising antitumor activity
Havrylyuk, Dmytro,Zimenkovsky, Borys,Lesyk, Roman,Vasylenko, Olexandr,Gzella, Andrzej
, p. 8630 - 8641,12 (2020/09/16)
The synthesis and antitumor activity screening of novel 3-[2-(3,5-diaryl-4,5-dihydropyrazol-1-yl)-4-oxo-4,5-dihydro-1, 3-thiazol-5-ylidene]-2,3-dihydro-1H-indol-2-ones 1-23 and 3-(3,5-diarylpyrazol- 1-yl)-2,3-dihydro-1H-indol-2-ones 24-39 are performed. I
Synthesis and anticancer activity of isatin-based pyrazolines and thiazolidines conjugates
Havrylyuk, Dmytro,Kovach, Natalya,Zimenkovsky, Borys,Vasylenko, Olexandr,Lesyk, Roman
scheme or table, p. 514 - 522 (2011/10/31)
The synthesis and antitumor activity screening of novel isatin based conjugates with thiazolidine and pyrazoline moieties were performed. Reaction of 3,5-diaryl-4,5-dihydropyrazoles with chloroacetyl chloride yielded starting 2-chloro-1-(3,5-diaryl-4,5-di
Synthesis and biological activity of some novel pyrazolines
Venkataraman, Setaraman,Jain, Saras,Shah, Kamal,Upmanyu, Neeraj
experimental part, p. 361 - 366 (2011/09/13)
Chalcones were prepared from substituted acetophenones and substituted benzaldehydes and condensed with hydrazine hydrate in ethanol to get the corresponding pyrazolines (Pdc1 to Pdc 14). The compounds were synthesized and characterizes by TLC, melting po
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.
