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Synthesis and cytotoxicity of pentacyclic triterpenes‐aniline nitrogen mustard derivatives
Author(s) -
Liu ChunMei,
Tian XiaoYan,
Su ChunHua,
Huang JiaYan,
Chu XiangWu,
Deng ShengPing,
Cheng KeGuang
Publication year - 2020
Publication title -
journal of the chinese chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.329
H-Index - 45
eISSN - 2192-6549
pISSN - 0009-4536
DOI - 10.1002/jccs.201900049
Subject(s) - chemistry , hela , cytotoxicity , ursolic acid , terpene , pharmacophore , aniline , oleanolic acid , stereochemistry , mtt assay , conjugate , nitrogen mustard , biochemistry , organic chemistry , in vitro , chromatography , medicine , mathematical analysis , alternative medicine , mathematics , surgery , pathology , chemotherapy , cyclophosphamide
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.