2393-17-1Relevant articles and documents
Irreversible enzyme inhibitors. CLXXIV. Metabolism of 4-(p-(4,6-diamino-1,2-dihydro-2,2-dimethyl-s-triazin-1-yl)hydrocinnamido)-o-toluenesulfonyl fluoride (NSC-113423), an active-site-directed irreversible inhibitor of dihydrofolic reductase.
Ryan,Vermeulen,Baker
, p. 1140 - 1142 (1970)
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Positive variation of the MRI signal via intramolecular inclusion complexation of a C-2 functionalized β-cyclodextrin
Zgani,Idriss,Barbot,Djeda?ni-Pilard,Petit,Hubert-Roux,Estour,Gouhier
supporting information, p. 564 - 569 (2017/01/25)
The synthesis of a new contrast agent based on a β-cyclodextrin scaffold and bearing a flexible lipophilic spacer arm on its secondary face is reported. Intermolecular host-guest inclusion complexes were known to undergo an enhancement of the contrast imaging. We extend this concept to intramolecular complexation. Inter- and intramolecular interactions are compared by NMR spectroscopy, circular dichroism and magnetic resonance imaging using hydrocinnamic acid and adamantane carboxylic acid as external guests. This positive variation of the observed relaxivity is a key element of new strategies aiming at developing smart molecular MRI probes.
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.
