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Chem. J. Chinese Universities

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Studies on the Synthesis and Cytotoxic Activities of 13-cis-Retinoyl Sugar Derivatives

XIANG Jian-Nan1,2,3*, CHEN Chao-Yue4, JIANG Li-Hui1, ZHOU Hou-Xiang1, YIN Kai1, DENG Xiao-Qiang1, CHEN Jing1, HE Xiao-Xiao2,3, WANG Ke-Min1,2,3   

    1. College of Chemistry and Chemical Engineering,
    2. Bio-medicine Engineering Center,
    3. State Key Laboratory of Chem/Biosensing and Chemometrics, Hunan University, Changsha 410082, China;
    4. Department of Chemical Engineering, Anhui University of Science and Technology, Huainan 232001, China
  • Received:2006-11-03 Revised:1900-01-01 Online:2007-08-10 Published:2007-08-10
  • Contact: XIANG Jian-Nan

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Abstract: In order to decrease the toxicities of retinoids and enhance the pharmaceutical effects, especially the cytotoxic activities, retinoic acids were modified by glycosyl groups. Nine new retinoyl sugar derivatives of 13-cis-retinoic acid(5a—5d, 6a, 10a—10c, 11a) were synthesized in good yields. Their structures were characterized and their cytotoxic activities were determined in vitro with MTT assay by using human cancer lines including A549 cells lines etc. The results show that glucoside derivatives exhibited interesting cytotoxic activities and their cytotoxic activities are stronger than glycosyl esters. Deactylation of compounds 5a and 10a also improved their bioactivities, respectively.

Key words: 13-cis-Retinoic acid, Retinoid, Glycosyl Ester, Cytotoxic activity

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