90649-82-4Relevant academic research and scientific papers
Sulfones nitroxyl radical as a radioprotective agent application
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Paragraph 0016-0017, (2018/05/16)
The invention discloses a sulfone-type nitroxide free radical represented by a structural general formula (I) and an application thereof as a radiation protectant. In the formula, R1 is absent or is halogen, C1-C3 alkyl, C1-C3 alkoxy or -CF3; and R2 is hy
Styryl sulfones compound, its preparation method and its use as neuroprotective agents
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Paragraph 0059-0061; 0080-0082, (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.
New compound with radiation protection function, preparation method and pharmaceutical application thereof
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Paragraph 0112; 0113; 0114, (2017/04/03)
The invention provides a new compound with a radiation protection function, and pharmaceutically acceptable salt, pro-drug and solvate. The compound and the pharmaceutically acceptable salt, pro-drug and solvate are as shown in formula (I): a chemical for
E-3,4-di-calcium method for preparing vinyl sulfoxide compound thereof as a neuroprotective pharmaceutical application
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Paragraph 0031-0033, (2017/01/12)
The invention relates to an application of E-3,4-dihydroxyphenylvinyl sulfoxide represented by the formula I in preparation of nerve protection drugs for treating neurodegenerative diseases, wherein the definitions of each group in the formula I are listed in the description. The invention also relates to a preparation method of E-3,4-dihydroxyphenylvinyl sulfoxide.
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.
Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7- oxo-7,8-dihydro-pyrido[2,3- d ]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5)
Reddy, M. V. Ramana,Akula, Balireddy,Cosenza, Stephen C.,Athuluridivakar, Saikrishna,Mallireddigari, Muralidhar R.,Pallela, Venkat R.,Billa, Vinay K.,Subbaiah, D. R. C. Venkata,Bharathi, E. Vijaya,Vasquez-Del Carpio, Rodrigo,Padgaonkar, Amol,Baker, Stacey J.,Reddy, E. Premkumar
, p. 578 - 599 (2014/03/21)
The success of imatinib, a BCR-ABL inhibitor for the treatment of chronic myelogenous leukemia, has created a great impetus for the development of additional kinase inhibitors as therapeutic agents. However, the complexity of cancer has led to recent interest in polypharmacological approaches for developing multikinase inhibitors with low toxicity profiles. With this goal in mind, we analyzed more than 150 novel cyano pyridopyrimidine compounds and identified structure-activity relationship trends that can be exploited in the design of potent kinase inhibitors. One compound, 8-cyclopentyl-2-[4-(4-methyl- piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6- carbonitrile (7x), was found to be the most active, inducing apoptosis of tumor cells at a concentration of approximately 30-100 nM. In vitro kinase profiling revealed that 7x is a multikinase inhibitor with potent inhibitory activity against the CDK4/CYCLIN D1 and ARK5 kinases. Here, we report the synthesis, structure-activity relationship, kinase inhibitory profile, in vitro cytotoxicity, and in vivo tumor regression studies by this lead compound.
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)-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.
ALPHA, BETA-UNSATURATED SULFOXIDES FOR TREATING PROLIFERATIVE DISORDERS
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Page/Page column 87; 88, (2008/06/13)
alphabeta-Unsaturated sulfoxides of Formula I: (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.
