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

doi:10.5246/jcps.2015.12.102

Abstract

Abstract:

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

CLC Number:

R916

Supporting:

Liang Guo, Wenxi Fan, Ziyun Gan, Wei Chen, Qin Ma, Rihui Cao. Design and synthesis of 1-substituted-β-carboline derivatives as potential anticancer agents[J]. Journal of Chinese Pharmaceutical Sciences, 2015, 24(12): 801-808.

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