Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines
Abstract
:1. Introduction
2. Results and Discussion
2.1. Chemistry
2.2. Cytotoxic Activity
Compd. | IC50 (μM) a | |||
---|---|---|---|---|
PC-3 b | LNCaP b | DU145 b | RWPE-1 b | |
5 | >50 | 27.85 ± 1.72 | >50 | >50 |
6 | >50 | 27.70 ± 4.17 | 28.92 ± 0.98 | 38.78 ± 0.77 |
7 | >50 | 31.22 ± 0.63 | >50 | 41.05 ± 0.54 |
8 | >50 | 26.60 ± 0.86 | 8.25 ± 0.16 | 31.69 ± 3.14 |
9 | >50 | 3.47 ± 0.36 | >50 | 31.01 ± 1.57 |
10 | >50 | 31.94 ± 0.89 | 47.75 ± 2.02 | >50 |
11 | >50 | >50 | >50 | >50 |
12 | >50 | 30.73 ± 0.83 | >50 | >50 |
13 | >50 | 28.27 ± 0.49 | >50 | >50 |
14 | >50 | >50 | >50 | 38.95 ± 0.77 |
15 | >50 | 1.25 ± 0.23 | >50 | 41.01 ± 0.47 |
16 | >50 | 32.47 ± 1.04 | >50 | >50 |
17 | >50 | 26.76 ± 1.00 | 26.83 ± 0.92 | 23.94 ± 0.75 |
18 | 26.89 ± 1.00 | 13.11 ± 0.51 | >50 | >50 |
19 | >50 | 26.58 ± 0.40 | >50 | 29.85 ± 0.80 |
20 | >50 | >50 | >50 | >50 |
21 | >50 | 25.28 ± 1.55 | >50 | >50 |
22 | >50 | 39.41 ± 0.54 | >50 | >50 |
23 | >50 | 33.25 ± 2.69 | >50 | 35.89 ± 1.25 |
24 | >50 | 19.85 ± 1.01 | >50 | >50 |
25 | >50 | 32.96 ± 0.21 | >50 | 18.94 ± 3.68 |
26 | >50 | 26.83 ± 1.51 | >50 | >50 |
27 | 24.95 ± 0.68 | >50 | >50 | 26.79 ± 3.01 |
28 | >50 | 18.21 ± 1.88 | 24.71 ± 2.22 | 28.46 ± 2.18 |
29 | >50 | 42.98 ± 7.58 | 38.23 ± 2.45 | 19.73 ± 0.01 |
naftopidil | 42.10 ± 0.79 | 22.36 ± 0.61 | 34.58 ± 0.31 | >50 |
3. Experimental Section
3.1. General Information
3.1.1. 2-(4-(Bromomethyl)phenyl)ethanol (2)
3.1.2. 2-(4-((Benzo[d][1,3]dioxol-5-yloxy)methyl)phenyl)ethanol (3)
3.1.3. 2-(4-((Benzo[d][1,3]dioxol-5-yloxy)methyl)phenyl)ethyl 4-methylbenzenesulfonate (4)
3.1.4. General Procedure for the Preparation of Compounds 5–29
3.2. In Vitro Cytotoxic Assay
3.2.1. Cell Culture
3.2.2. Assessment of Antitumor Activity by CCK-8 Assay
4. Conclusions
Acknowledgments
Author Contributions
Conflicts of Interest
References
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Chen, H.; Liang, X.; Xu, F.; Xu, B.; He, X.; Huang, B.; Yuan, M. Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines. Molecules 2014, 19, 12048-12064. https://doi.org/10.3390/molecules190812048
Chen H, Liang X, Xu F, Xu B, He X, Huang B, Yuan M. Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines. Molecules. 2014; 19(8):12048-12064. https://doi.org/10.3390/molecules190812048
Chicago/Turabian StyleChen, Hong, Xue Liang, Fang Xu, Bingbing Xu, Xuelan He, Biyun Huang, and Mu Yuan. 2014. "Synthesis and Cytotoxic Activity Evaluation of Novel Arylpiperazine Derivatives on Human Prostate Cancer Cell Lines" Molecules 19, no. 8: 12048-12064. https://doi.org/10.3390/molecules190812048