Journal of Chinese Pharmaceutical Sciences ›› 2015, Vol. 24 ›› Issue (12): 801-808.DOI: 10.5246/jcps.2015.12.102

• Original articles • Previous Articles     Next Articles

Design and synthesis of 1-substituted-β-carboline derivatives as potential anticancer agents

Liang Guo1, Wenxi Fan1, Ziyun Gan1, Wei Chen1, Qin Ma1, Rihui Cao2*   

  1. 1. Xinjiang Huashidan Pharmaceutical Research Co., Ltd., Urumqi 830011, China
    2. School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China
  • Received:2015-08-30 Revised:2015-09-23 Online:2015-12-22 Published:2015-09-30
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  • Supported by:

    National Science and Technology Major Project of  the Ministry of Science and Technology of China (Grant No. 2011ZX09401-007); National Key Technology Research and Development Program of the Ministry of Science and Technology of China (Grant No. 2012BAI30B00).


In the present study, we designed and synthesized a series of 1-substituted-β-carboline derivatives through modification of position-1, 2 and 9 of β-carboline nucleus in order to discover novel leading compounds with better antitumor activities and less toxicity. Their structures were confirmed by 1H NMR, 13C NMR, MS, IR and elemental analyses. All the target compounds were tested for cytotoxic activity against six cancer cell lines, including Bel-7402, HepG2, A549, A375, 786-0 and HT-29 by methyl thiazolyl tetrazolium (MTT) method. Studies of structure-activity relationships indicated that the effects of substituents in position-1 on cytotoxic activities were in an order as follows: 2-thienyl >2-chlorophenyl >4-chlorophenyl >benzyl group.

Key words: β-Carboline, Synthesis, Anticancer activity, Structure-activity relationships

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