Carbamates of 4'-demethyl-4-deoxypodophyllotoxin: synthesis, cytotoxicity and cell cycle effects |
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| Authors: | Chen Shi-Wu Gao Yuan-Yu Zhou Ni-Ni Liu Jie Huang Wen-Ting Hui Ling Jin Yan Jin Yong-Xin |
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| Institution: | aSchool of Pharmacy, State Key Laboratory of Applied Organic Chemistry, Key Lab of Preclinical Study for New Drugs of Gansu Province, Lanzhou University, Lanzhou 730000, China;bCollege of Chemical Engineering, Qingdao University of Science and Technology, Qingdao 266042, China;cExperimental Center of Medicine and Key Laboratory of Stem Cells and Gene Drug of Gansu Province, General Hospital of Lanzhou Military Command, Lanzhou 730050, China;dDepartment of Medicine, Second People’s Hospital of Gansu Province, Lanzhou 730000, China |
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| Abstract: | In an attempt to generate compounds with superior bioactivity and reduced toxicity, 12 carbamates of 4′-demethyl-4-deoxypodophyllotoxin, N-(1-oxyl-4′-demethyl- 4-deoxypodophyllic)-α-amino acids amides, were synthesized and evaluated for antiproliferative activity and cell cycle effects. These synthesized compounds proved to be more hydrophilic, as well as improved or comparable in vitro cytotoxicities against four cell lines (A-549, HeLa, SiHa, and HL-60) compared with either parent DPT or anti-cancer drug VP-16. Furthermore, flow cytometric analysis exhibited that N-(1-oxyl-4′-demethyl-4-deoxypodophyllic)-d-α-methine amide (15f) induced cell cycle arrest in the G2/M phase in A-549 cells. |
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| Keywords: | Podophyllotoxin 4-Deoxypodophyllotoxin Amino acid Antitumor activity |
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