Journal
RSC ADVANCES
Volume 9, Issue 72, Pages 42509-42515Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c9ra08665j
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Funding
- National Natural Science Foundation of China [81502921, 81530091, 81673317, 81602979]
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A novel geldanamycin-ferulic acid conjugate LZY228 was prepared and evaluated for anti-proliferation activity on human cancer cell line MDA-MB-231. Compound LZY228 exhibited potent cytotoxicity with IC50 value of 0.27 mu M, which was more potent than 17-AAG. Hepatotoxicity test in mice demonstrated that the levels of both AST and ALT of LZY228-treated group were lower than that of GA-treated group, indicating that LZY228 was a promising antitumor candidate. In addition, excellent in vivo antitumor potency of LZY228 was observed in MDA-MB-231 xenograft model, which was superior to reference drug 17-AAG. Docking and MD refinement of the Hsp90-LZY228 complex give us an explanation of theoretical binding model of 17-ferulamido-17-demethoxygeldanamycins at molecular level.
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