Synthesis and stability evaluation of 5-FU-acetic podophyllic ester as anti-tumor agent

Abstract

Abstract:

Aim To study a new anti-cancer drug 5-FU-acetic podophyllic ester derivatized from podophyllotoxin. Methods A novel derivative of podophyllotoxin was synthesized. Its inhibitory effects against P-388, A-549, Bel-7402 and HL-60 in vitro were tested. The stability tests under different kinds of conditions were carried out. Results The novel derivative showed stronger inhibitory activities against P-388, A-549 and Bel-7402 in vitro than VP-16. The novel derivative was found to be stable at 60 ℃ and 4500 lx light in solid-state, but was less stable in humid condition. It was more stable in methanol (4 ℃) and chloroform (25 ℃) than in methanol (25 ℃), and less stable in artificial gastric juice(AGJ, 37 ℃). Its stabilities were decreased while increasing the pH of buffer solutions. Conclusion These results could provide useful information for further study of this compound.

Key words: Podophyllotoxin, Podophyllotoxin, 5-Fluorouracil, 5-Fluorouracil, Anti-tumor activity, Anti-tumor activity, Stabilities, Stabilities

CLC Number:

R916

Supporting:

Rong Xiang, Fu-Min Zhang, Jing-Man Ni^*, Xuan Tian. Synthesis and stability evaluation of 5-FU-acetic podophyllic ester as anti-tumor agent[J]. .

References

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