5334-31-6Relevant articles and documents
Quantitative analysis and alkaline stability studies of allopurinol.
Gressel,Gallelli
, p. 335 - 338 (1968)
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Synthesis, anticancer evaluation, and molecular docking studies of some novel 4,6-disubstituted pyrazolo[3,4-d]pyrimidines as cyclin-dependent kinase 2 (CDK2) inhibitors
Cherukupalli, Srinivasulu,Chandrasekaran, Balakumar,Kry?tof, Vladimír,Aleti, Rajeshwar Reddy,Sayyad, Nisar,Merugu, Srinivas Reddy,Kushwaha, Narva Deshwar,Karpoormath, Rajshekhar
, p. 46 - 59 (2018/05/23)
A novel series of 4,6-disubstituted pyrazolo[3,4-d]pyrimidines (7–43) bearing various anilines at C-4 position and thiophenethyl or thiopentane moieties at C-6 position have been designed and synthesized by molecular hybridization approach. All the synthesized compounds were evaluated for in vitro CDK2/cyclin E and Abl kinase inhibitory activity as well as anti-proliferative activity against K-562 (chronic myelogeneous leukemia), and MCF-7 (breast adenocarcinoma) cell lines. The structure–activity relationship (SAR) studies revealed that compounds with thiophenethyl group at C-6 with mono-substituted anilines at C-4 exhibited better CDK2 inhibitory activity compared to alkyl group (thiopentane) at C-6 and di-substituted anilines at C-4 of the scaffold. In particular, compounds having 2-chloro, 3-nitro and 4-methylthio aniline groups at C-4 displayed significant enzymatic inhibitory activity against CDK2 with single digit micromolar IC50 values. The in silico molecular docking studies suggested possible binding orientation and the binding energies were in agreement with the observed SAR as well as experimental results. In addition, some of the synthesized compounds showed anti-proliferative effects against K-562 and MCF-7 cancer cell lines with IC50 values in a micromolar range. Thus, the synthesized compounds could be considered as new anticancer hits for further lead optimization.
Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines
Ouyang, Xiaohu,Piatnitski, Evgueni L.,Pattaropong, Vatee,Chen, Xiaoling,He, Hai-Ying,Kiselyov, Alexander S.,Velankar, Avdhoot,Kawakami, Joel,Labelle, Marc,Smith II, Leon,Lohman, Julia,Lee, Sui Ping,Malikzay, Asra,Fleming, James,Gerlak, Jason,Wang, Ying,Rosler, Robin L.,Zhou, Kai,Mitelman, Stan,Camara, Margarita,Surguladze, David,Doody, Jacqueline F.,Tuma, M. Carolina
, p. 1191 - 1196 (2007/10/03)
Oxadiazole derivatives were synthesized and evaluated for their ability to inhibit tubulin polymerization and to cause mitotic arrest in tumor cells. The most potent compounds inhibited tubulin polymerization at concentrations below 1 μM. Lead analogs caused mitotic arrest of A431 human epidermoid cells and cells derived from multi-drug resistant tumors (10, EC50 = 7.8 nM). Competition for the colchicine binding site and pharmacokinetic properties of selected potent compounds were also investigated and are reported herein, along with structure-activity relationships for this novel series of antimitotic agents.