MedChemComm
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Journal Name
DOI: 10.1039/C4MD00573B
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Conclusions
In conclusion, we described the discovery and
optimization
10.
of
Nꢀ(4ꢀphenylthiazolꢀ2ꢀyl)
cinnamamide
derivatives as novel potential antiꢀtumor agents. These
compounds were synthesized and evaluated for their antiꢀ
cancer activities in vitro. The SAR analysis showed that
conformational restriction and steric effect played a crucial role
on the antiꢀproliferation activities. The most potent analogue 8f
displayed excellent inhibitory activities against several human
cancer cell lines at subꢀmicromolar to nanomolar
concentrations, including K562, Bel7402, A549, MV4ꢀ11 and
Jurkat, while no apparent toxicity to nonꢀcancerous cells was
observed. The further studies of the mechanism of action
implied that 8f might display its antiꢀcancer activity via
inducing apoptosis, which was worthy of developing as an antiꢀ
cancer candidates.
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13.
14.
15.
16.
In brief, our results provided interesting information for
the design of novel Nꢀ(4ꢀphenylthiazolꢀ2ꢀyl) cinnamamide
derivatives with better antiꢀcancer potency. Further studies on
the exact biological mechanisms and antiꢀtumor research in
vivo are underway.
17.
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Acknowledgements
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We thank Lei Li of State Key Laboratory of Biotherapy
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Notes and references
a Sichuan University, State Key Laboratory of Biotherapy/Collaborative
Innovation Center of Biotherapy and Cancer Center, West China Hospital,
West China Medical School, Sichuan University, Chengdu 610041, China. b
Department of Pharmaceutical and Bioengineering, School of Chemical
Engineering, Sichuan University, Chengdu, Sichuan 610065, China. c College
of Chemistry and Life Science, Chengdu Normal University, Chengdu
611130, China. d Department of Encephalopathy, The First Affiliated
Hospital of Henan University of Traditional Chinese Medicine, Henan
University of Traditional Chinese Medicine, Zhengzhou, 450004,China. e
Wisdom Pharmaceutical Co., Ltd, Haimen, 226123,China.
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‡These authors contributed equally to this work.
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