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Mar. Drugs 2016, 14(5), 85; doi:10.3390/md14050085

Novel Azetidine-Containing TZT-1027 Analogues as Antitumor Agents

School of Pharmacy, Fudan University, Shanghai 201203, China
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Authors to whom correspondence should be addressed.
Academic Editor: Patrizia Diana
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)
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Abstract

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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MDPI and ACS Style

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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