scholarly journals Synthesis and Cytotoxic Activity of Novel Betulin Derivatives Containing Hydrazide-Hydrazone Moieties

2021 ◽  
Vol 16 (10) ◽  
pp. 1934578X2110553
Author(s):  
Jiale Wu ◽  
Jiafeng Wang ◽  
Yinglong Han ◽  
Yu Lin ◽  
Jing Wang ◽  
...  

A series of novel betulin derivatives containing hydrazide-hydrazone moieties were synthesized. All compounds were evaluated for their cytotoxicity against four human carcinoma cell lines (HepG2, A549, MCF-7 and HCT-116) and a normal human gastric epithelial cell line (GES-1). Among them, compound 6i was the most potent against HepG2 and MCF-7 cell lines, with IC50 values of 9.27 and 8.87 μM, respectively. The results suggest that the incorporation of a hydrazide-hydrazone side chain at the C-28 position of betulin is beneficial for compounds to display significant cytotoxicity. Compound 6i may be used as a promising skeleton for antitumor agents with improved efficacy.

2019 ◽  
Vol 16 (6) ◽  
pp. 462-467
Author(s):  
Songtao Li ◽  
Hongling Zhao ◽  
Zhifeng Yin ◽  
Shuhua Deng ◽  
Yang Gao ◽  
...  

A series of new phenanthrene-based tylophorine derivatives (PBTs) were synthesized in good yield and their structures were characterized by 1H-NMR spectroscopy and ESI MS. In vitro antitumor activity of these compounds against five human carcinoma cell lines, including HCT116 (colorectal), BGC-823 (gastric), HepG-2 (hepatic), Hela (cervical) and H460 (lung) cells, was evaluated by MTT assay. Among these PBTs, compound 6b showed the highest antitumor activities against HCT116 and HepG-2 cell lines with IC50 values of 6.1 and 6.4 μM, respectively, which were comparable to that of adriamycin hydrochloride. The structure-activity relationship of these compounds was also discussed based on the results of their antitumor activity.


Cell Calcium ◽  
1984 ◽  
Vol 5 (3) ◽  
pp. 309
Author(s):  
Gaby E. Pfyffer ◽  
Gisela Haemmerli ◽  
Peter Sträuli ◽  
Claus W. Heizmann

Cancer ◽  
1995 ◽  
Vol 75 (9) ◽  
pp. 2262-2268 ◽  
Author(s):  
Jannifer S. Stromberg ◽  
Yong J. Lee ◽  
Elwood P. Armour ◽  
Alvaro A. Martinez ◽  
Peter M. Corry

1996 ◽  
Vol 16 (1) ◽  
pp. 53-60 ◽  
Author(s):  
Elisa A. Spillare ◽  
Aikou Okamoto ◽  
Koichi Hagiwara ◽  
Douglas J. Demetrick ◽  
Manuel Serrano ◽  
...  

Oncogene ◽  
2000 ◽  
Vol 19 (4) ◽  
pp. 514-525 ◽  
Author(s):  
Torsten E Reichert ◽  
Shigeki Nagashima ◽  
Yoshiro Kashii ◽  
Joanna Stanson ◽  
Gui Gao ◽  
...  

2007 ◽  
Author(s):  
Judith Bergs ◽  
Jaap Haveman ◽  
Rosemarie Ten Cate ◽  
Jan Medema ◽  
Nicolaas Franken ◽  
...  

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