Literature DB >> 23459613

Discovery of O-Alkylamino Tethered Niclosamide Derivatives as Potent and Orally Bioavailable Anticancer Agents.

Haijun Chen1, Zhengduo Yang, Chunyong Ding, Lili Chu, Yusong Zhang, Kristin Terry, Huiling Liu, Qiang Shen, Jia Zhou.   

Abstract

Niclosamide has been identified to potently inhibit the activation, nuclear translocation, and transactivation of STAT3. Nevertheless, the poor aqueous solubility and bioavailability of niclosamide has hindered its further clinical development for cancer therapy. To discover new molecules with enhanced drug-like properties, a series of novel O-alkylamino tethered derivatives of niclosamide have been designed, synthesized, and biologically evaluated. Among them, compound 11 (HJC0152) has been demonstrated to significantly suppress MDA-MB-231 xenograft tumor growth in vivo (i.p. & p.o.), indicating its great potential as efficacious and orally bioavailable therapeutics for human cancer.

Entities:  

Keywords:  Niclosamide derivatives; STAT3; orally bioavailable; water solubility

Year:  2013        PMID： 23459613      PMCID： PMC3583367          DOI： 10.1021/ml3003082

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  35 in total

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Authors:  Sina Haftchenary; Miriam Avadisian; Patrick T Gunning
Journal:  Anticancer Drugs       Date:  2011-02       Impact factor: 2.248

Review 8.  STATs in cancer inflammation and immunity: a leading role for STAT3.

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  38 in total

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