Facile Synthesis, Cytotoxicity and Inhibition on Telomerase of Symmetrical Uvariadiamide Analogues
[1]
Dan Wang, School of Pharmacy, Jiangsu University, Zhenjiang, China.
[2]
Jian Tang, School of Pharmacy, Jiangsu University, Zhenjiang, China.
[3]
Jianke Feng, School of Pharmacy, Jiangsu University, Zhenjiang, China.
[4]
Yongsheng Jin, School of Pharmacy, Second Ministry Medical University, Shanghai, China.
[5]
Haisheng Chen, School of Pharmacy, Second Ministry Medical University, Shanghai, China.
[6]
Min Wang, College of Material and Chemistry, Chemical Engineering, Hangzhou Normal University, Hangzhou, China.
[7]
Michael B. Jarstfer, Eshelman School of Pharmacy, UNC Chapel Hill, North Carolina, USA.
Symmetrical uvariadiamide analogues were facially synthesized and evaluated for their cytotoxic activities. The 4-methxoy analogues exhibited significant cytotoxicity against HCT116 and A549 cells, and compound 13c had an IC50 of 0.69 μg/mL against A549 cell. The 4-NH2 analogues showed slight inhibition on the two cell lines. Compounds 9b, 11b and 12b from 1,4-butanediamine showed remarkable cytotoxic effect, while compounds 9a, 9c, 11a, 11c, 12a and 12c with a chain of two or six carbon atoms had feeble inhibition on the cell lines. Both of the substituted groups and carbon chains between nitrogen atoms were important to the inhibition of uvariadiamide analogues. The cytotoxic compounds have no obvious inhibition on the telomerase.
Uvariamicrocarpa, N, N'-Butane-1, 4-Diylbis(4-Methoxybenzamide), Uariadiamide Analogues, Cytotoxicity, Telomerase
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