28203-60-3Relevant academic research and scientific papers
Synthesis, characterization, and radioprotective activity of α,β-unsaturated aryl sulfone analogs and their Tempol conjugates
Zhou, Nan,Feng, Tian,Shen, Xin,Cui, Jiahui,Wu, Rangxin,Wang, Libin,Wang, Siwang,Zhang, Shengyong,Chen, Hui
supporting information, p. 1063 - 1068 (2017/07/12)
Some novel α,β-unsaturated aromatic sulfone analogs (5a-5m) and their Tempol conjugates (6a-6e) have been synthetically prepared, characterized and evaluated for their radioprotective activity under γ-ray radiation. The Tempol conjugates were characterize
Styryl sulfones compound, its preparation method and its use as neuroprotective agents
-
Paragraph 0063-0065; 0142-0144, (2018/02/04)
The application relates to design of a novel molecule with ester group substituted by sulfone group by using a caffeic acid phenethyl ester (CAPE) with neuroprotective activity extracted from natural propolis as a primer according to bioisosterism principle and hydrogen-bond interaction theory; and the molecule has a structural general formula I, and the definition of each group is shown in the claims. The invention also relates to compound in vitroantioxidation capability evaluation, neuroprotective activity evaluation on cell level and traverse blood brain barrier ability evaluation. Activity evaluation results show that the synthesized novel compound has enhanced neuroprotective activity and can easily traverse the blood brain barrier, thus becoming a novel neuroprotective agent for treating neurodegenerative diseases.
Synthesis and antioxidant activity of 1,4-[Bis(3-arylmethanesulfonyl pyrrolyl and pyrazolyl)]benzenes
Lavanya, Gopala,Padmavathi, Venkatapuram,Padmaja, Adivireddy
, p. 1200 - 1207 (2014/08/05)
A variety of (1,4-phenylene)bis(arylmethanesulfonylpyrroles and pyrazoles) were prepared by the cycloaddition of 1,3-dipolar reagents, tosylmethyl isocyanide and diazomethane to the Michael acceptor, 1,4-bis(E)-2- ((arylmethanesulfonyl)vinyl)benzene. All the compounds were evaluated for antioxidant activity. Amongst the tested compounds, one of them displayed excellent radical scavenging activity in all the three methods evaluated when compared with the standard Ascorbic acid. On the other hand, 1,4-(bis(3-arylmethanesulfonyl)-1H-pyrazol-4-yl)benzenes exhibited comparatively higher antioxidant activity than 1,4-(bis(3-arylmethanesulfonyl)-1H-pyrrol-4- yl) benzenes. In general, it was observed that compounds having methoxy substitutent on aromatic ring displayed greater antioxidant activity than the other substituents. ?2014 Sociedade Brasileira de Qui?mica.
Design, synthesis, and biological evaluation of (E)-3,4-dihydroxystyryl aralkyl sulfones and sulfoxides as novel multifunctional neuroprotective agents
Ning, Xianling,Guo, Ying,Wang, Xiaowei,Ma, Xiaoyan,Tian, Chao,Shi, Xueqi,Zhu, Renzong,Cheng, Can,Du, Yansheng,Ma, Zhizhong,Zhang, Zhili,Liu, Junyi
, p. 4302 - 4312 (2014/06/09)
Novel (E)-3,4-dihydroxystyryl aralkyl sulfones and sulfoxides were designed and synthesized as new analogues of 1, which showed interesting multifunctional neuroprotective effects, including antioxidative and antineuroinflammatory properties. Specifically, target compounds display excellent potency in scavenging reactive free radicals and demonstrate potent effects against various kinds of toxicities, including H2O2, 6-hydroxydopamine, and lipopolysaccharide in different types of neuronal cells. The antioxidative properties of the target compounds are more potent than that of 1, and the antineuroinflammatory properties are less strong than that of 1. According to the parallel artificial membrane permeation assay for the blood-brain barrier, target compounds possess greater blood-brain barrier (BBB) permeability than 1. In short, due to improvement of the antioxidative effect, stability, and BBB permeability, (E)-3,4-dihydroxystyryl aralkyl sulfones and sulfoxides can thus be considered as potential multifunctional neuroprotective agents and serve as new lead candidates in the treatment of neurodegenerative diseases.
Design, synthesis, and biological evaluation of (E)-styrylbenzylsulfones as novel anticancer agents
Reddy, M. V. Ramana,Mallireddigari, Muralidhar R.,Cosenza, Stephen C.,Pallela, Venkat R.,Iqbal, Nabisa M.,Robell, Kimberly A.,Kang, Anthony D.,Reddy, E. Premkumar
, p. 86 - 100 (2008/09/20)
Cell cycle progression is regulated by cyclins and cyclin-dependent kinases, which are formed at specific stages of the cell cycle and regulate the G1/S and G2/M phase transitions, employing a series of "checkpoints" governed by phosphorylation of their substrates. Tumor development is associated with the loss of these checkpoint controls, and this provides an approach for the development of therapeutic agents that can specifically target tumor cells. Here, we describe the synthesis and SAR of a novel group of cytotoxic molecules that selectively induce growth arrest of normal cells in the G1 phase while inducing a mitotic arrest of tumor cells resulting in selective killing of tumor cell populations with little or no effect on normal cell viability. The broad spectrum of antitumor activity in vitro and xenograft models, lack of in vivo toxicity, and drug resistance suggest potential for use of these agents in cancer therapy.
