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Short Paper | Special issue | Vol 97, No. 1, 2018, pp.560-568
Published online, 1st March, 2018
DOI: 10.3987/COM-18-S(T)25
Synthesis of N-ω-Phenylalkyl-4-(p-chlorophenyl)-piperidin-4-ol Analogues with Potent Antiproliferative Activity Against HCT-116 Cells

Noriyuki Hatae,* Eiko Kujime, Keigo Yano, Mami Kizuka, Rina Ashida, Tominari Choshi, Takashi Nishiyama, Chiaki Okada, Tatsunori Iwamura, and Teruki Yoshimura*

*Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido, Ishikari-Tobetsu, Hokkaido 061-0293, Japan

Abstract

Some opioid analogues, such as morphine and loperamide, were reported to exhibit weak antiproliferative activity against tumor cells. In a study of loperamide analogues, we found that adding an N-ω-phenylalkyl group onto the 4-arylpiperidin-4-ol unit can have important effects on the antiproliferative activity of such compounds against HCT-116 cells. We optimized the distance between the phenyl group and 4-arylpiperidin unit to promote such activity.