Synthesis and Biological Evaluation of Novel Betulin Derivatives with Aromatic Hydrazone Side Chain as Potential Anticancer Agents

A series of novel betulin-28-hydrazone derivatives (7a-7o) were synthesized. All compounds were evaluated for their in vitro cytotoxicities in four human carcinoma cells (HepG2, MCF-7, HCT-116 and A549). Among them, compound 7l displayed the most potent cytotoxicity with an IC50 (concentration of th...

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Published inJournal of the Brazilian Chemical Society Vol. 33; no. 3; pp. 227 - 237
Main Authors Wang, Jiafeng, Wu, Jiale, Han, Yinglong, Zhang, Jie, Lin, Yu, Wang, Haijun, Wang, Jing, Bu, Ming
Format Journal Article
LanguageEnglish
Published SAO PAULO Soc Brasileira Quimica 01.03.2022
Sociedade Brasileira de Química
Subjects
Chemistry
CHEMISTRY, MULTIDISCIPLINARY
Physical Sciences
Science & Technology
IN-VITRO
ACID
heterocycles
antitumor
apoptosis
betulin derivatives
hydrazone
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Summary:A series of novel betulin-28-hydrazone derivatives (7a-7o) were synthesized. All compounds were evaluated for their in vitro cytotoxicities in four human carcinoma cells (HepG2, MCF-7, HCT-116 and A549). Among them, compound 7l displayed the most potent cytotoxicity with an IC50 (concentration of the tested compound that inhibits 50% of cell growth) value of 7.37 +/- 0.38 mu M against MCF-7 cells. The preliminary cellular mechanism studies indicated that compound 7l could induce MCF-7 cells apoptosis. The above findings indicated that compound 7l may be used as a lead compound for antitumor agents with improved efficacy.
ISSN:0103-5053
1678-4790
1678-4790
DOI:10.21577/0103-5053.20210140