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Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone |
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| Authors: | Kung Pei-Pei Funk Lee Meng Jerry Collins Michael Zhou Joe Zhongxiang Johnson M Catherine Ekker Anne Wang Jeff Mehta Pramod Yin Min-Jean Rodgers Caroline Davies Jay F Bayman Eileen Smeal Tod Maegley Karen A Gehring Michael R |
| Institution: | Pfizer Global Research and Development, La Jolla Laboratories, 10770, Science Center Dr., San Diego, CA 92121, USA. peipei.kung@pfizer.com |
| Abstract: | Information from X-ray crystal structures were used to optimize the potency of a HTS hit in a Hsp90 competitive binding assay. A class of novel and potent small molecule Hsp90 inhibitors were thereby identified. Enantio-pure compounds 31 and 33 were potent in PGA-based competitive binding assay and inhibited proliferation of various human cancer cell lines in vitro, with IC(50) values averaging 20 nM. |
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