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Open AccessArticle

Design, Synthesis, and Biological Evaluation of Novel Nitrogen Heterocycle-Containing Ursolic Acid Analogs as Antitumor Agents

School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, China
*
Authors to whom correspondence should be addressed.
Authors contributed equally.
Molecules 2019, 24(5), 877; https://doi.org/10.3390/molecules24050877
Received: 21 January 2019 / Revised: 17 February 2019 / Accepted: 19 February 2019 / Published: 1 March 2019
(This article belongs to the Special Issue Heterocycles in Medicinal Chemistry)
Nineteen ursolic acid analogues were designed, synthesized, and evaluated for their antiproliferative activity against the Hela and MKN45 cell lines. Some compounds containing a piperazine moiety displayed moderate to high levels of antitumor activities against the tested cancer cell lines. The most potent compound shares the IC50 value of 2.1 µM and 2.6 µM for the Hela and MKN45 cell lines, respectively. Further mechanism studies and in vivo antitumor studies have shown that it decreased the apoptosis regulator (BCL2/BAX) ratio, disrupted mitochondrial potential and induced apoptosis, and suppressed the growth of Hela xenografts in nude mice. View Full-Text
Keywords: ursolic acid analogues; synthesis; nitrogen heterocycles; apoptosis; antitumor activity ursolic acid analogues; synthesis; nitrogen heterocycles; apoptosis; antitumor activity
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MDPI and ACS Style

Wang, W.; Lei, L.; Liu, Z.; Wang, H.; Meng, Q. Design, Synthesis, and Biological Evaluation of Novel Nitrogen Heterocycle-Containing Ursolic Acid Analogs as Antitumor Agents. Molecules 2019, 24, 877. https://doi.org/10.3390/molecules24050877

AMA Style

Wang W, Lei L, Liu Z, Wang H, Meng Q. Design, Synthesis, and Biological Evaluation of Novel Nitrogen Heterocycle-Containing Ursolic Acid Analogs as Antitumor Agents. Molecules. 2019; 24(5):877. https://doi.org/10.3390/molecules24050877

Chicago/Turabian Style

Wang, Wenzhi; Lei, Lei; Liu, Zhi; Wang, Hongbo; Meng, Qingguo. 2019. "Design, Synthesis, and Biological Evaluation of Novel Nitrogen Heterocycle-Containing Ursolic Acid Analogs as Antitumor Agents" Molecules 24, no. 5: 877. https://doi.org/10.3390/molecules24050877

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