5959-36-4Relevant articles and documents
Fluorescence PET (photo-induced electron transfer) sensor for water based on anthracene-amino acid
Ooyama, Yousuke,Matsugasako, Ai,Nagano, Tomoya,Oka, Kazuyuki,Kushimoto, Kohei,Komaguchi, Kenji,Imae, Ichiro,Harima, Yutaka
, p. 52 - 55 (2011)
An anthracene-amino acid system with two carboxyl groups has been designed and synthesized as a new class of fluorescence PET (photo-induced electron transfer) sensor for detection of water in organic solvents. An enhancement in fluorescence is observed with increasing water content in 1,4-dioxane, THF, acetonitrile and ethanol, which is attributable to the suppression of PET by the intramolecular proton transfer of the carboxyl proton to the amino group. The detection limit and quantitation limit are, respectively, 0.1 and 0.3 wt% for 1,4-dioxane, 0.4 and 1.2 wt% for THF, 0.1 and 0.3 wt% for acetonitrile and 0.1 and 0.3 wt% for ethanol.
Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma
Zhou, Ruolan,Fang, Shaoyu,Zhang, Minmin,Zhang, Qingsen,Hu, Jian,Wang, Mingping,Wang, Chongqing,Zhu, Ju,Shen, Aijun,Chen, Xin,Zheng, Canhui
supporting information, p. 349 - 352 (2019/01/04)
Multiple myeloma (MM) is the second most common haematological malignancy. Almost all patients with MM eventually relapse, and most recommended treatment protocols for the patients with relapsed refractory MM comprise a combination of drugs with different mechanisms of action. Therefore novel drugs are in urgent need in clinic. Bcl-2 inhibitors and HDAC inhibitors were proved their anti-MM effect in clinic or under clinical trials, and they were further discovered to have synergistic interactions. In this study, a series of Bcl-2/HDAC dual-target inhibitors were designed and synthesized. Among them, compounds 7e–7g showed good inhibitory activities against HDAC6 and high binding affinities to Bcl-2 protein simultaneously. They also displayed good growth inhibitory activities against human MM cell line RPMI-8226, which proved their potential value for the treatment of multiple myeloma.
Design, synthesis, and potent antiepileptic activity with latent nerve rehabilitation of novel γ-aminobutyric acid derivatives
He, Dian,Ma, Jing,Shi, Xiuxiao,Zhao, Chunyan,Hou, Meng,Guo, Qingxin,Ma, Shangxian,Li, Xiaojun,Zhao, Peicheng,Liu, Wenhu,Yang, Zhuqing,Mou, Jianping,Song, Pengfei,Zhang, Yang,Li, Jing
, p. 967 - 978 (2015/02/19)
We aimed to design and synthesize novel γ-aminobutyric acid (GABA) derivatives with the combination of aspirin (ASA) of nerve rehabilitative pharmacophores so as to develop multifunctional drugs useful in the treatment of neurological disorders. Twenty-four novel esters and amides of 1a were synthesized, biologically evaluated for antiepileptic activity with the model of 4-aminopyridine (4-AP), and tested for their capacity of penetrating the blood-brain barrier (BBB) with HPLC. The distribution of 8a, ASA freed by 8a, 7c, and ASA freed by 7c within 24 h in brain tissue was measured. The structure-activity relationship (SAR) was established and the data of Computer Aided Drug Design (CADD) showed good results. With ED50 values of, 0.3684-0.5199 mmol/kg, LD50 1.1487-1.3944 mmol/kg, and therapeutic index (TI) 2.65-3.15, compounds 8a, 3b, 4b, 6c, and 7c exhibited better antiepileptic activities in multiples of 0.3 to 2.2 against the control sodium valproate (VPA). Most importantly, 8a and 7c exhibited excellent antiepileptic activities with TI values of, 3.15 and 3.12, respectively.
