期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 4, 期 2, 页码 180-185出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml3003082
关键词
niclosamide derivatives; STAT3; water solubility; orally bioavailable
资金
- National Institute of Health [P50 CA097007, P30DA028821, R21MH093844]
- R. A. Welch Foundation Chemistry and Biology Collaborative Grant from Gulf Coast Consortia (GCC)
- John Sealy Memorial Endowment Fund
- Duncan Family Institute (DFI)
- MD Anderson Cancer Center
Niclosamide has been identified to potently inhibit the activation, nuclear translocation, and transactivation of STAT3. Nevertheless, the poor aqueous solubility and bioavailability of niclosamide have hindered its further clinical development for cancer therapy. To discover new molecules with enhanced druglike 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 (ip and po), indicating its great potential as efficacious and orally bioavailable therapeutics for human cancer.
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