CRCU

Chemical Research in Chinese Universities ›› 2004, Vol. 20 ›› Issue (3): 299-304.

• Articles • Previous Articles     Next Articles

Syntheses of 2- or 6-Substituted Chromones and Chromone Ring-opening Reaction in Polyphosphoric Acid

HE Xun-gui1,2, YOU Qi-dong1, LI Zhi-yu1   

  1. 1. Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, P. R. China;
    2. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, P. R. China
  • Received:2003-07-01 Online:2004-06-24 Published:2011-08-06
  • Supported by:

    Supported by the Excellent Backbone Young Teacher Foundation of Ministry of Education of China and the Natural Science Foundation of Jiangsu Province(No.BK2001079).

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Abstract: In an attempt to find new antitumor agents, a novel class of chromone compounds with a benzimidazole or a benzoxazole ring in positions 2 or 6 were synthesized via condensation in polyphosphoric acid(PPA) by using chromone acids as the starting materials. During the preparation process, it was found that PPA could cleave the chromone ring to produce a ring-opening compound(6). The molar ratio of the chromone compound(5) to the ring-opening compound(6) varied with the change of reaction temperature and time. Based on MTT protocol, the antitumor activity of each of the compounds obtained was evaluated against three human cancer cell lines: KB(oral epidermal), A2780(ovary) and Bel7402(liver). The IC50 varied from 54.7 μmol/L to more than 180 μmol/L.

Key words: 2- or 6-Substituted chromone, Antitumor agent, Polyphosphoric acid, Ring-opening reaction