41964-65-2Relevant articles and documents
Novel monoacylglycerol lipase inhibitor as well as preparation method and application thereof
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Paragraph 0264-0266, (2021/02/10)
The invention discloses a novel monoacylglycerol lipase inhibitor as well as a preparation method and application thereof. Specifically, the invention provides a compound shown as a formula I, or a pharmaceutically acceptable salt, a stereoisomer, or a deuterated derivative thereof. Experimental results show that the compound provided by the invention can effectively inhibit MAGL activity, can beused for preparing an MAGL inhibitor and preparing medicines for preventing and/or treating diseases (including endometrial cancer, colorectal cancer, liver cancer, breast cancer, ovarian cancer, neurodegenerative diseases and the like) related to abnormal MAGL activity, and has a wide application prospect.
Synthesis and Cytotoxic Evaluation of Some New 1,2,3-Triazole Linked 2-Imino-4-(Trifuoromethyl)-Thiazolidin-4-ol Derivatives
Appalanaidu, K.,Dadmal, Tulshiram L.,Kumbhare, Ravindra M.,Pamanji, R.,Rao, J. Venkateswara,Reddy, Prathyusha J.,Velatooru, L. R.
, p. 81 - 89 (2021/08/12)
A new series of 1,2,3-triazole tagged 2-imino-4-(trifluoromethyl)thiazolidinol derivatives was synthesized through click chemistry under Sharpless conditions and evaluated for anticancer activity against human monocytic leukemia (U937), human breast adeno
Design, synthesis of novel (Z)-2-(3-(4-((3-benzyl-2,4-dioxothiazolidin-5-ylidene)methyl)-1-phenyl-1H-pyrazol-3-yl)phenoxy)-N-arylacetamide derivatives: Evaluation of cytotoxic activity and molecular docking studies
Kolluri, Prashanth Kumar,Gurrapu, Nirmala,Subhashini,Putta, Shravani,Singh, Surya Sathyanarayana,Vani, Tamalapakula,Manga, Vijjulatha
, (2019/11/26)
In an attempt to discover potential cytotoxic agents, a series of novel (Z)-2-(3-(4-((3-benzyl-2,4-dioxothiazolidin-5-ylidene)methyl)-1-phenyl-1H-pyrazol-3-yl) phenoxy)-N-arylacetamide derivatives 11a-n were synthesized in varied steps with acceptable reaction procedures with good yields and characterized by 1H NMR, 13C NMR, IR and ESI-MS spectra. All the novel synthesized derivatives were assessed for their cytotoxic activity against human breast cell line (MCF-7) with different concentration of 0.625 μM, 1.25 μM, 2.5 μM, 5 μM and 10 μM respectively. Biological evaluation assay results were displayed in terms of percentage of cell viability reduction and IC50 values. Most of the screened derivatives demonstrated moderate to promising cytotoxic activity. Some of the derivatives, particularly compound 11d and 11n have shown promising cytotoxic activity with IC50 values 0.604 μM and 0.665 μM compared to standard drug cisplatin and compounds 11a, 11e and 11g also have shown considerable cytotoxic activity and the rest of the derivatives have shown moderate activity. Furthermore, molecular docking calculations and ADME properties of the synthesized molecules are in effective compliance with the cytotoxic evaluation results.