Literature DB >> 31012734

Design, synthesis, and cytotoxic activities of novel hybrids of parthenolide and thiazolidinedione via click chemistry.

Jie Qiu1,2,3, Chun-Mao Yuan1,2,3, Min Wen1,3, Ya-Nan Li1,2,3, Juan Chen1,2,3, Jun-You Jian1,2,3, Lie-Jun Huang1,2,3, Wei Gu1,2,3, Yan-Mei Li1,2,3, Xiao-Jiang Hao1,2,3,4.   

Abstract

A series of novel parthenolide-thiazolidinedione hybrids have been synthesized via a click chemistry-mediated coupling between parthenolide and thiazolidinedione, and evaluated for their cytotoxic activities. The results indicated that all the hybrids showed moderate cytotoxic effects on human cancer cell lines, including human erythroleukemia cell line (HEL), prostate (PC3), and breast (MDA-MB-231) by MTT assay. In particular, compound VI-6 exhibited the best cytotoxic activities against the MDA-MB-231 cells with IC50 value of 2.07 µM, which was about eight times more active than that of the original compound (PTL). These interesting results might be used to develop novel lead scaffolds for potential anticancer agents.

Entities:  

Keywords:  Parthenolide–thiazolidinedione hybrids; click chemistry; cytotoxic activities

Year:  2019        PMID: 31012734     DOI: 10.1080/10286020.2019.1597055

Source DB:  PubMed          Journal:  J Asian Nat Prod Res        ISSN: 1028-6020            Impact factor:   1.569


  1 in total

Review 1.  Recent Advances in Bioactive Flavonoid Hybrids Linked by 1,2,3-Triazole Ring Obtained by Click Chemistry.

Authors:  Daniela Pereira; Madalena Pinto; Marta Correia-da-Silva; Honorina Cidade
Journal:  Molecules       Date:  2021-12-30       Impact factor: 4.411

  1 in total

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