Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 48, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2021.128233
Keywords
Heterocyclic; Dihydropyrazole; Anticancer activity; Mechanism
Categories
Funding
- National Natural Science Foundation of China [81960754]
- Yunnan Provincial Science and Technology Department-Applied Basic Research Joint Special Funds of Yunnan University of Chinese Medicine [202001AZ070001-007, 202001AZ070001-038, 2020FF002(-005), 2017FF117(-041), 2018FF001 (009)]
- Yunnan Applicative and Basic Research Program [2018FY001001, 202001AU070116]
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In this study, a series of novel heterocyclic substituted dihydropyrazole derivatives were synthesized, among which piperazine substituted compounds showed superior anticancer activity. Particularly, compound 4o was found to induce G2/M arrest in HCC1806 cells and significantly accumulate p21 protein, demonstrating potent antitumor activity.
In this work, a series of novel heterocyclic substituted dihydropyrazole derivatives have been prepared, and in vitro anticancer activity against a panel of human tumor cell lines by SRB were evaluated. The results indicated that piperazine substituted dihydropyrazole derivatives exhibited superior anticancer activity than that of other compounds. Especially, compounds 4g, 4h, 4l, 4m, 4o, 6g, 6j and 6l showed potent antitumor activity. Further mechanism study demonstrated that compound 4o could induce G2/M arrest in HCC1806 cell and p21 accumulation significantly.
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