Lead optimization of dual tubulin and Hsp27 inhibitors

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Lead optimization of dual tubulin and Hsp27 inhibitors.

Tubulin and heat shock protein 27 (Hsp27) are well-characterized molecular targets for anti-cancer drug development. We previously identified lead compounds that inhibited both Hsp27 and tubulin. These compounds exhibited extensive anti-cancer activities against the proliferation of various human cancer cell lines. In the current study, a systematic ligand based structural optimization led to n...

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The expression of heat shock protein 27 (Hsp27) as a chaperone protein, is increased in response to various stress stimuli such as anticancer chemotherapy. This phenomenon can lead to survive of the cells and causes drug resistance. In this study, a series of methanesulfonamide derivatives as dual Hsp27 and tubulin inhibitors in the treatment of cancer were applied to quantitative structure–act...

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ژورنال

عنوان ژورنال: European Journal of Medicinal Chemistry

سال: 2014

ISSN: 0223-5234

DOI: 10.1016/j.ejmech.2014.04.038