15118-60-2Relevant articles and documents
Moffett,Vaughan
, p. 1238 (1960)
P-aminobenzene butyric acid preparation method
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Paragraph 0023; 0042; 0044, (2017/07/21)
The invention relates to a P-aminobenzene butyric acid preparation method. According to the method, alkyl-acyl aniline serves as raw materials, dichloroethane serves as a reaction solvent, a compound A is prepared by the aid of acylation reaction and acetone water recrystallization modes, P-aminobenzene butyric acid is prepared by the aid of Huang Minglong reaction according to the weight ratio of a solvent S and the compound A of 1:1, and the highest yield of end products reach 98%. The method cannot generate solid waste difficult to being treated and is environmentally friendly and stable in process and suitable for industrial production and high in yield, the purity of the prepared P-aminobenzene butyric acid is good, and the method assists in normal stable production of chlorambucil.
Design, synthesis and biological evaluation of novel sesquiterpene mustards as potential anticancer agents
Xu, Yuan-Zhen,Gu, Xue-Yan,Peng, Shou-Jiao,Fang, Jian-Guo,Zhang, Ying-Mei,Huang, De-Jun,Chen, Jian-Jun,Gao, Kun
, p. 284 - 297 (2015/03/30)
Several novel series of sesquiterpene mustards (SMs) bearing nitrogen mustard and glutathione (GSH)-reactive α-methylene-γ-butyrolactone groups were successfully prepared for the first time and showed excellent antiproliferative activities in vitro. Among them, compounds 2e and 2g displayed the highest antiproliferative properties with IC50 values ranging from 2.5 to 8.7 μM. The selectivity of these two compounds was evaluated by SRB method against human cancer and normal hepatic cells (HepG2 and L02). The induction of apoptosis and effects on the cell cycle distribution with compounds 2e and 2g were investigated by Hoechst 33,258 staining and flow cytometry, which exhibited that they could induce selective cell apoptosis and cell cycle arrest in HepG2 and L02 cells. In addition, further investigation showed that compounds 2e and 2g could obviously inhibit the proliferation of HepG2 cells by inducing significant DNA cross-linking and depleting GSH in cell media. The good cytotoxicity and selectivity of compounds 2e and 2g pointed them as promising leads for anticancer drug design.