475115-23-2Relevant academic research and scientific papers
Dihydropyrazothiazole derivatives as potential MMP-2/MMP-8 inhibitors for cancer therapy
Wang, Zhong-Chang,Shen, Fa-Qian,Yang, Meng-Ru,You, Ling-Xia,Chen, Li-Zhi,Zhu, Hai-Liang,Lu, Ya-Dong,Kong, Fan-Lei,Wang, Ming-Hua
, p. 3816 - 3821 (2018)
MMP-2/MMP-8 is established as one of the most important metalloenzymes for targeting cancer. A series of dihydropyrazothiazole derivatives (E1–E18) bearing a salicylaldehyde group linked to Pyrazole ring were designed, synthesized, and evaluated for their pharmacological activity as MMP-2/MMP-8 inhibitors. Among them, compound E17 exhibited most potent inhibitory activity (IC50 = 2.80 μM for MMP-2 and IC50 = 5.6 μM for MMP-8), compared to the positive drug CMT-1 (IC50 = 1.29 μM). Compounds (E1–E18) were scrutinized by CoMFA and CoMSIA techniques of Three-dimensional quant. structure-activity relationship (3D-QSAR), as well as a docking simulation. Moreover, treatment with compound E4 could induce MCF-7 cell apoptosis. Overall, the biological profile of E1–E18 may provide a research basis for the development of new agents against cancer.
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 of novel thiazolone-based compounds containing pyrazoline moiety and evaluation of their anticancer activity
Havrylyuk, Dmytro,Zimenkovsky, Borys,Vasylenko, Olexandr,Zaprutko, Lucjusz,Gzella, Andrzej,Lesyk, Roman
scheme or table, p. 1396 - 1404 (2009/07/04)
To examine the anticancer activity several novel thiazolone-based compounds containing 5-aryl-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl framework were obtained. Reaction of 5-aryl-3-phenyl-4,5-dihydropyrazole with 4-thioxo-2-thiazolidinone or 2-carbethoxymethy
Substituted pyrazolines and their cardiovascular activity
Malhotra, Vineet,Pathak, Seema,Nath, Rajendra,Mukerjee, Devashis,Shanker, Kirpa
, p. 1310 - 1313 (2007/10/03)
1-Thiocarbamoyl-3, 5-diphenyl-2-pyrazolines 4 and 5 have been prepared by cyclization of 1,3-diphenyl-2-propene-1 ones (chalcones) 3 with thiosemicarbazide in the presence of sodium hydroxide. Reaction of 3 with hydrazine hydrate followed by condensation with aryl isothiocyanates yields 1-N-substituted thiocarbamoyl-3, 5-diphenyl-2-pyrazolines 5. These compounds have been characterized on the basis of elemental analysis, IR, 1H NMR and MS. Compounds have been evaluated for their cardio-vascular activity and toxicity.
