876724-22-0Relevant academic research and scientific papers
Design and synthesis of a new series of 3,5-disubstituted-1,2,4-oxadiazoles as potential colchicine binding site inhibitors: Antiproliferative activity, molecular docking, and SAR studies
Abdel-Aal, Eatedal H.,Abdel-Sami, Zakaria K.,Abo-Dya, Nader E.,Al-Karmalawy, Ahmed A.,Diab, Rana T.
, p. 21657 - 21669 (2021/12/09)
The development of anticancer compounds targeting the colchicine-binding site of tubulin, termed colchicine-binding site inhibitors (CBSIs) is a promising research area for pharmaceutical companies and research institutes. A series of 3,5-disubstituted 1,
Compounds containing a 1,2,4-oxadiazole ring, and preparation method thereof, and applications in immunosuppressive drugs
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Paragraph 0124-0125; 0128-0132; 0137, (2020/01/12)
The invention belongs to the field of organic synthesis and pharmaceutical chemistry drugs, and relates to a preparation method of a class of compounds containing a 1,2,4-oxadiazole ring and having astructural general formula represented by (I), and appli
Design and Synthesis of Marine Phidianidine Derivatives as Potential Immunosuppressive Agents
Liu, Jin,Li, Heng,Chen, Kai-Xian,Zuo, Jian-Ping,Guo, Yue-Wei,Tang, Wei,Li, Xu-Wen
, p. 11298 - 11308 (2019/01/04)
A series of novel marine phidianidine derivatives were designed, synthesized, and evaluated for their immunosuppressive activities during our search of potential immunosuppressive agents with high efficacy and low toxicity from marine sources. These compounds were tested for their inhibitory activity on Con A-induced T cell and lipopolysaccharide-induced B cell proliferation. Compounds 14a and 18c, displaying the most promising inhibitory effects and low toxicities, were further found to possess immune-regulatory activities upon cross-linking of T cell receptor (TCR) and B cell receptor (BCR) on purified T and B cells, respectively.
Synthesis of novel 1,2,4-oxadiazoles and analogues as potential anticancer agents
Kumar, Dalip,Patel, Gautam,Chavers, Angela K.,Chang, Kuei-Hua,Shah, Kavita
, p. 3085 - 3092 (2011/07/08)
A library of 3,5-disubstituted-1,2,4-oxadiazoles 7-9 and their bioisosters, 1,3,4-oxadiazole 14 and 1,3,4-thiadiazole 16, were synthesized and evaluated in vitro for their anticancer potential against a panel of six human cancer cell lines. The key step in the synthesis of oxadiazoles 7-9 involve coupling of amidoxime 6 with an appropriate carboxylic acid followed by thermal cyclization. The bioisosteres, 1,3,4-oxadiazole 14 and 1,3,4-thiadiazole 16 were prepared from the reaction of a common precursor diacylhydrazine 13 with thionyl chloride and Lawesson′s reagent, respectively. The anticancer studies on the synthesized compounds revealed that presence of a cyclopentyloxy or n-butyloxy on the C-3 aryl ring and piperdin-4-yl or trichloromethyl at the C-5 position of 1,2,4-oxadiazole is essential for good activity. In particular, 1,2,4-oxadiazole 7i and analogue 1,3,4-thiadiazole 16 exhibited significant activity against DU145 (IC50: 9.3 μM) and MDA-MB-231 (IC 50: 9.2 μM) cell lines, respectively.
