Design, synthesis, anticancer activity and cytotoxicity of novel 4-piperidone/cyclohexanone derivatives

Design, synthesis, anticancer activity and cytotoxicity of novel 4-piperidone/cyclohexanone... Qin Chen and Yun Hou have contributed equally to this work. & Gui-Ge Hou guigehou@163.com & Chun-Hua Wang chunhuawang508@126.com The Key Laboratory of Prescription Effect and Clinical Evaluation of State Administration of Traditional Chinese Medicine of China, Binzhou Medical University, Yantai 264003, People’s Republic of China 123 8120 Q. Chen et al. Keywords 4-Piperidone  Cyclohexanone  Schiff-base  Anticancer activity Cytotoxicity Introduction Curcumin (Diferuloylmethane, Fig. 1), a member of the curcuminoid family, is the yellow-coloured phenolic pigment of the rhizome of Curcuma longa or turmeric from the Zingiberaceae family. Since antiquity, Curcuma longa or turmeric has been used to improve colour and flavor of food products [1, 2]. More important, curcumin, the active principle of turmeric [3, 4], has been reported to possess anti- inflammatory, anticoagulant, antibacterial, antifungal, anticarcinogenic, antitumor, anti-HIV, anti-mutagenic, antiproliferative, antioxidant, anti-protozoal, and anti- venom activities [5–10]. Curcumin and its analogues containing the pharmacophore of 1,5-diaryl-3-oxo-1,4-pentadienyl, is thought to interact at the primary binding site and bio-thiols from susceptible neoplasms. The pharmacophore of methoxyphenol groups align at an auxiliary site and also influence their bio-activities. However, curcumin and some analogues have many major problems in clinical applications, such as poor aqueous solubility, relatively low bioavailability, http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Research on Chemical Intermediates Springer Journals

Design, synthesis, anticancer activity and cytotoxicity of novel 4-piperidone/cyclohexanone derivatives

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Publisher
Springer Netherlands
Copyright
Copyright © 2016 by Springer Science+Business Media Dordrecht
Subject
Chemistry; Catalysis; Physical Chemistry; Inorganic Chemistry
ISSN
0922-6168
eISSN
1568-5675
D.O.I.
10.1007/s11164-016-2583-y
Publisher site
See Article on Publisher Site

Abstract

Qin Chen and Yun Hou have contributed equally to this work. & Gui-Ge Hou guigehou@163.com & Chun-Hua Wang chunhuawang508@126.com The Key Laboratory of Prescription Effect and Clinical Evaluation of State Administration of Traditional Chinese Medicine of China, Binzhou Medical University, Yantai 264003, People’s Republic of China 123 8120 Q. Chen et al. Keywords 4-Piperidone  Cyclohexanone  Schiff-base  Anticancer activity Cytotoxicity Introduction Curcumin (Diferuloylmethane, Fig. 1), a member of the curcuminoid family, is the yellow-coloured phenolic pigment of the rhizome of Curcuma longa or turmeric from the Zingiberaceae family. Since antiquity, Curcuma longa or turmeric has been used to improve colour and flavor of food products [1, 2]. More important, curcumin, the active principle of turmeric [3, 4], has been reported to possess anti- inflammatory, anticoagulant, antibacterial, antifungal, anticarcinogenic, antitumor, anti-HIV, anti-mutagenic, antiproliferative, antioxidant, anti-protozoal, and anti- venom activities [5–10]. Curcumin and its analogues containing the pharmacophore of 1,5-diaryl-3-oxo-1,4-pentadienyl, is thought to interact at the primary binding site and bio-thiols from susceptible neoplasms. The pharmacophore of methoxyphenol groups align at an auxiliary site and also influence their bio-activities. However, curcumin and some analogues have many major problems in clinical applications, such as poor aqueous solubility, relatively low bioavailability,

Journal

Research on Chemical IntermediatesSpringer Journals

Published: May 27, 2016

References

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