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Open AccessArticle

Novel Azetidine-Containing TZT-1027 Analogues as Antitumor Agents

School of Pharmacy, Fudan University, Shanghai 201203, China
Authors to whom correspondence should be addressed.
Academic Editor: Patrizia Diana
Mar. Drugs 2016, 14(5), 85;
Received: 30 March 2016 / Revised: 21 April 2016 / Accepted: 22 April 2016 / Published: 28 April 2016
(This article belongs to the Special Issue Synthesis of Antitumor Marine Alkaloids and Related Analogues)
PDF [1676 KB, uploaded 28 April 2016]


A conformational restriction strategy was used to design and synthesize nine TZT-1027 analogues. 3-Aryl-azetidine moiety was used to replace phenylethyl group of TZT-1027 at the C-terminus. These analogues exhibited moderate to excellent antiproliferative activities, and the most potent compound 1a showed IC50 values of 2.2 nM against A549 and 2.1 nM against HCT116 cell lines, respectively. However, 1a could not achieve effective inhibition at all the dose levels in the A549 xenograft model (up to 5 mg/kg, injection, once a day), which is only 16%–35% inhibition at the end of the experiment. View Full-Text
Keywords: TZT-1027; azetidine; conformation restriction; antiproliferative activity TZT-1027; azetidine; conformation restriction; antiproliferative activity

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Yan, Q.; Wang, Y.; Zhang, W.; Li, Y. Novel Azetidine-Containing TZT-1027 Analogues as Antitumor Agents. Mar. Drugs 2016, 14, 85.

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