Synthesis and cytotoxicity of pentacyclic triterpenes-aniline nitrogen mustard derivatives |
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Authors: | Chun-Mei Liu Xiao-Yan Tian Chun-Hua Su Jia-Yan Huang Xiang-Wu Chu Sheng-Ping Deng Ke-Guang Cheng |
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Institution: | State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmacy, Guangxi Normal University, Guilin, P. R. China |
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Abstract: | To discover novel nitrogen mustards, the reported mustard pharmacophore was combined with natural pentacyclic triterpenes, which are characterized with pharmacological and structural diversity. Thus, six conjugates were synthesized with 1,2,3-triazole linking N,N-bis (2-chloroethyl)-1,4-phenylenediamine and oleanolic acid, ursolic acid, or glycyrrhetinic acid, and their biological activity was evaluated against tumor cell lines HeLa, BGC-823, BEL-7404, and NCI-H460 using the MTT assay. As a result, these conjugates showed some selective cytotoxicity to NCI-H460, though all their activity potency was moderate or weak in the four cell lines. |
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Keywords: | N N-bis (2-chloroethyl)-1 4-phenylenediamine nitrogen mustards pentacyclic triterpenes |
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