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2018 | 75 | 5 | 1135-1145
Article title

NEW BETULIN NITRATES: SYNTHESIS, CYTOTOXIC ACTIVITY AND MOLECULAR DOCKING EVALUATION

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Languages of publication
EN
Abstracts
EN
Betulin and its derivatives have been reported to affect several key genes of cell-cycle regulators. However, their specific targets haven’t yet been discovered. As an important cell cycle regulator, Cyclin-dependent kinase-2 (CDK2) has become a potential target for cancer therapy. Here we describe the design, synthesis and antitumor activities in vitro of eleven new betulin nitrates. The results revealed that compound (20) possesses potent antitumor activity against MCF-7 cell lines (IC50 < 10 μM). In order to investigate potential protein target, betulin nitrates were subjected to docking studies with CDK2. Compound (20) showed very good binding affinity for CDK2 via hydrogen bonding interactions. Thus, the CDK2 inhibitory potential could make compound (20) possible candidate as antitumor agent.
Year
Volume
75
Issue
5
Pages
1135-1145
Physical description
Dates
published
2018-10-31
Contributors
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author
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References
Document Type
Publication order reference
Identifiers
YADDA identifier
bwmeta1.element.doi-10_32383_appdr_81731
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