370096-68-7Relevant academic research and scientific papers
Development of a sphingosine kinase 1 specific small-molecule inhibitor
Hengst, Jeremy A.,Wang, Xujun,Sk, Ugir H.,Sharma, Arun K.,Amin, Shantu,Yun, Jong K.
, p. 7498 - 7502 (2010)
The sphingolipid metabolic pathway represents a potential source of new therapeutic targets for numerous hyperproliferative/inflammatory diseases. Targets such as the sphingosine kinases (SphKs) have been extensively studied and numerous strategies have b
Synthesis of new bis-pyrazole linked hydrazides and their in vitro evaluation as antimicrobial and anti-biofilm agents: A mechanistic role on ergosterol biosynthesis inhibition in Candida albicans
Khan, Irfan,Kanugala, Sirisha,Shareef, Mohd. Adil,Ganapathi, Thipparapu,Shaik, Anver Basha,Shekar, Kunta Chandra,Kamal, Ahmed,Kumar, Chityal Ganesh
, p. 1339 - 1351 (2019/04/30)
Literature reports suggest that pyrazoles and hydrazides are potential antimicrobial pharmocophores. Considering this fact, a series of nineteen conjugates containing hybrids of bis-pyrazole scaffolds joined through a hydrazide linker were synthesized and
Pyrazole-oxadiazole conjugates: Synthesis, antiproliferative activity and inhibition of tubulin polymerization
Kamal, Ahmed,Shaik, Anver Basha,Polepalli, Sowjanya,Santosh Reddy, Vangala,Bharath Kumar,Gupta, Soma,Rama Krishna,Nagabhushana, Ananthamurthy,Mishra, Rakesh K.,Jain, Nishant
, p. 7993 - 8007 (2015/02/18)
A number of pyrazole-oxadiazole conjugates were synthesized and evaluated for their ability to function as antiproliferative agents on various human cancer cell lines. These conjugates are comprised of pyrazole and oxadiazole scaffolds closely attached to each other without any spacer as two structural classes. The Type I class has a trimethoxy substituent and the type II class has a 3,4-(methylenedioxy) substituent on their A rings. Among these conjugates, 11a, 11d and 11f manifest potent cytotoxicity with IC50values ranging from 1.5 μM to 11.2 μM and inhibit tubulin polymerization with IC50values of 1.3 μM, 3.9 μM and 2.4 μM respectively. The cell cycle assay showed that treatment with these conjugates results in accumulation of cells in the G2/M phase and disrupts the microtubule network. Elucidation of zebrafish embryos revealed that the conjugates cause developmental defects. Molecular docking simulations determined the binding modes of these potent conjugates at the colchicine site of tubulin.
Synthesis, X-ray crystal structure and optical properties of novel 5-(3-aryl-1H-pyrazol-5-yl)-2-(6-methoxy-3-methylbenzofuran-2-yl)-1,3, 4-oxadiazole
Jiang, Zhen-Ju,Liu, Jin-Ting,Lv, Hong-Shui,Zhao, Bao-Xiang
scheme or table, p. 181 - 186 (2012/01/15)
A series of novel 5-(3-aryl-1H-pyrazol-5-yl)-2-(6-methoxy-3- methylbenzofuran-2-yl)-1,3,4-oxadiazole derivatives has been synthesized from 6-methoxy-3-methylbenzofuran-2-carboxylic acid and ethyl 3-aryl-1H-pyrazole-5- carboxylate. The structures of compou
