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Synthesis and antitumor activity of natural compound aloe emodin derivatives. 2015
Naraganahalli R Thimmegowda, and
Chanmi Park, and
Bettaswamigowda Shwetha, and
Krisada Sakchaisri, and
Kangdong Liu, and
Joonsung Hwang, and
Sangku Lee, and
Sook J Jeong, and
Nak K Soung, and
Jae H Jang, and
In-Ja Ryoo, and
Jong S Ahn, and
Raymond L Erikson, and
Bo Y Kim
World Class Institute (WCI), Incurable Diseases Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang, Cheongwon, 363-883, Korea; Department of Chemistry, Govt.S K S J T Institute, Bangalore, Karnataka, 560001, India.
In this study, we have synthesized novel water soluble derivatives of natural compound aloe emodin 4(a-j) by coupling with various amino acid esters and substituted aromatic amines, in an attempt to improve the anticancer activity and to explore the structure-activity relationships. The structures of the compounds were determined by (1) H NMR and mass spectroscopy. Cell growth inhibition assays revealed that the aloe emodin derivatives 4d, 4f, and 4i effectively decreased the growth of HepG2 (human liver cancer cells) and NCI-H460 (human lung cancer cells) and some of the derivatives exhibited comparable antitumor activity against HeLa (Human epithelial carcinoma cells) and PC3 (prostate cancer cells) cell lines compared to that of the parent aloe emodin at low micromolar concentrations.
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