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α-Trifluoromethyl Chalcones as Potent Anticancer Agents for Androgen Receptor-Independent Prostate Cancer |
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| Authors: | Yohei Saito Atsushi Mizokami Kouji Izumi Renato Naito Masuo Goto Kyoko Nakagawa-Goto |
| Institution: | 1.School of Pharmaceutical Sciences, College of Medical, Pharmaceutical and Health Science, Kanazawa University, Kanazawa 920-1192, Japan;2.Department of Integrative Cancer Therapy and Urology, School of Medical Sciences, Kanazawa University, Kanazawa 920-1192, Japan; (K.I.); (R.N.);3.Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA; |
| Abstract: | α-Trifluoromethyl chalcones were prepared and evaluated for their antiproliferative activities against androgen-independent prostate cancer cell lines as well as five additional types of human tumor cell lines. The most potent chalcone 5 showed superior antitumor activity in vivo with both oral and intraperitoneal administration at 3 mg/kg. Cell-based mechanism of action studies demonstrated that 5 induced cell accumulation at sub-G1 and G2/M phases without interfering with microtubule polymerization. Furthermore, several cancer cell growth-related proteins were identified by using chalcone 5 as a bait for the affinity purification of binding proteins. |
| Keywords: | chalcone trifluoromethyl group prostate cancer antitumor activity target proteins |