Synthesis and antitumor activity of novel CDDO derivatives

PEI Jianghong; XIAO Yu; Li Qixing; ZHAO Zihao; CHEN Li

doi:10.11665/j.issn.1000-5048.20170507

Journal of China Pharmaceutical University > 2017 > 48(5): 548-553. > DOI: 10.11665/j.issn.1000-5048.20170507

PEI Jianghong, XIAO Yu, Li Qixing, ZHAO Zihao, CHEN Li. Synthesis and antitumor activity of novel CDDO derivatives[J]. Journal of China Pharmaceutical University, 2017, 48(5): 548-553. DOI: 10.11665/j.issn.1000-5048.20170507

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Synthesis and antitumor activity of novel CDDO derivatives

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Twelve novel 2-cyano-3, 12-dioxooleana-1, 9(11)-dien-28-oic acid(CDDO)derivatives were designed and synthesized( 9a - 9l )by introducing different heterocyclic rings to 17-COOH of CDDO through various linkers. Their structures were determined by ESI-MS, IR and ¹H NMR. The antiproliferative activity of the synthetic derivatives against human cancer cells HCT-116, A549 and HepG2 was evaluated by MTT assay. Several compounds showed potent inhibitory activities against test cell lines. Among them, compound 9c showed more potent antiproliferative activity than the CDDO-imidazolide(CDDO-Im). Moreover, rat plasma stability assay showed that compound 9c was more stable than CDDO-Im.
- CDDO,
- derivative,
- synthesis,
- antiproliferative activity,
- plasma stability

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