832-58-6Relevant articles and documents
Phloroglucinol derivatives as anti-tumor agents: synthesis, biological activity evaluation and molecular docking studies
Zhang, Fuli,Lai, Qingfu,Lai, Weihong,Li, Ming,Jin, Xiaobao,Ye, Lianbao
, p. 165 - 176 (2021/12/02)
Phloroglucinol compounds isolated from Dryopteris fragrans (L.) Schott showed a variety of biological activities, such as anticancer and anti-inflammatory. In this study, we have made a number of modifications around the scaffold of phloroglucinol and synthesized phloroglucinol derivatives A1–A9, B1–B9, and C1–C3. We synthesized these compounds and investigated their effect on four human cancer cell lines (A-549, MCF-7, Hela, HepG2 cell lines) via MTT assay in vitro. The results revealed that all compounds exhibited certain antiproliferative activities on cancer cell lines and excellent inhibitory effects on MCF-7, in which compound C2 was the best with the IC50 value of 18.49 μM, exceeding that of 5-fluorouracil. Moreover, the cell apoptosis test showed that compound C2 induced apoptosis in a concentration-dependent manner. Furthermore, the results of molecular docking analysis explained the probable interaction between the active compounds and active sites of target protein 4I22 and 1OG5. [Figure not available: see fulltext.]
Construction and Biological Evaluation of Small Libraries Based on the Intermediates within the Total Synthesis of Uvaretin
Perera, Shashika,Fernando, Asantha,Dallman, Johnathan,Weeramange, Chamitha,Lansakara, Ashabha,Nguyen, Thi,Rafferty, Ryan J.
, p. 1631 - 1639 (2021/04/29)
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Synthetic method for portulacanone D and anti-inflammatory pharmaceutical compounds containing thereof
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Paragraph 0060; 0061, (2019/10/08)
Inventors of the present invention synthesized natural homoisoflavonoid portulacanone D (compound 6) isolated from Portulaca oleracea L (POL). An ability to inhibit NO production in LPS-induced RAW 264.7 macrophages was assessed as an indicator of anti-inflammatory activity. The tested portulacanone D did not show clear cytotoxicity and inhibited NO production in the RAW 264.7 macrophages in a concentration dependent manner. The portulacanone D exhibits 92.5% of NO production inhibition at 10 andmu;M and has an IC50 value of 2.09 andmu;M. The finding has additional correlation with the suppressed expression of iNOS induced by LPS. According to the information obtained from the study of the present invention, the portulacanone D can be used in the development of anti-inflammatory drugs targeting NO production.COPYRIGHT KIPO 2019