排序方式: 共有119条查询结果,搜索用时 15 毫秒
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Tsutomu Akama Charlotte Virtucio Chen Dong Richard Kimura Yong-Kang Zhang James A. Nieman Rashmi Sharma Xiaosong Lu Marcelo Sales Rajeshwar Singh Anne Wu Xiao-Qing Fan Liang Liu Jacob J. Plattner Kurt Jarnagin Yvonne R. Freund 《Bioorganic & medicinal chemistry letters》2013,23(6):1680-1683
A series of novel 6-(aminomethylphenoxy)benzoxaborole analogs was synthesized for the investigation of the structure–activity relationship of the inhibition of TNF-alpha, IL-1beta, and IL-6, from lipopolysaccharide stimulated peripheral blood mononuclear cells. Compounds 9d and 9e showed potent activity against all three cytokines with IC50 values between 33 and 83 nM. Chloro substituted analog 9e (AN3485) is considered to be a promising lead for novel anti-inflammatory agent with a favorable pharmacokinetic profile. 相似文献
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Watkins WJ Lemoine RC Chong L Cho A Renau TE Kuo B Wong V Ludwikow M Garizi N Iqbal N Barnard J Jankowska R Singh R Madsen D Lolans K Lomovskaya O Oza U Dudley MN 《Bioorganic & medicinal chemistry letters》2004,14(20):5133-5137
Structure-activity relationships of a novel series of fungal efflux pump inhibitors with respect to potentiation of the activity of fluconazole against strains of Candida albicans and Candida glabrata over-expressing ABC-type efflux pumps are systematically explored. 相似文献
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Anticarcinogenic effects of hexaamminecobalt(III) chloride in mice initiated with diethylnitrosamine
Hexaamminecobalt(III) chloride ([Co(NH3)6]Cl3) was investigated for its antineoplastic role in relation to tumor marker enzymes, drug metabolizing enzymes, oxidative stress-related
parameters, and histopathological analysis of liver and lung tissues of mice. Initiation was performed using a single intraperitoneal
injection of diethylnitrosamine (DENA) at a carcinogenic dose of 90 mg/kg body weight. The cobalt complex supplementation
at a dose of 100 ppm in drinking water was given ad libitum throughout the experimental period of 14 weeks. In comparison
to lung, the cobalt complex supplementation was found to reverse DENA-induced biochemical changes more effectively in liver.
Histological examination of liver and lung from DENA-initiated and cobalt-complex-supplemented mice showed considerable protection
in the case of liver compared to that of lung. The involvement of the [Co(NH3)6]Cl3 in modulating several factors associated with carcinogenesis induced by DENA thus showed its anticarcinogenic potential against
chemically induced hepatocarcinogenesis. 相似文献
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Ram Reddy T Srinivasula Reddy L Rajeshwar Reddy G Nuthalapati VS Lingappa Y Sandra S Kapavarapu R Misra P Pal M 《Bioorganic & medicinal chemistry letters》2011,21(21):6433-6439
A multi component based synthesis involving palladium catalyzed C-C bond forming reaction has been developed as a new strategy to access systematically modified functionalized 2-aminochromenes. This MCR involves the use of bromobenzaldehyde as a key component and is highlighted by generating a new compound library. Many of these compounds showed Mycobacterium tuberculosis H37Rv chorismate mutase inhibiting properties in vitro representing the lead example of chorismate mutase inhibition by heteroarene based compounds. 相似文献
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Solar ultraviolet radiation-induced DNA damage in aquatic organisms: potential environmental impact 总被引:11,自引:0,他引:11
Continuing depletion of stratospheric ozone and subsequent increases in deleterious ultraviolet (UV) radiation at the Earth's surface have fueled the interest in its ecological consequences for aquatic ecosystems. The DNA is certainly one of the key targets for UV-induced damage in a variety of aquatic organisms. UV radiation induces two of the most abundant mutagenic and cytotoxic DNA lesions, cyclobutane pyrimidine dimers (CPDs) and pyrimidine pyrimidone photoproducts (6-4PPs) and their Dewar valence isomers. However, aquatic organisms have developed a number of repair and tolerance mechanisms to counteract the damaging effects of UV on DNA. Photoreactivation with the help of the enzyme photolyase is one of the most important and frequently occurring repair mechanisms in a variety of organisms. Excision repair, which can be distinguished into base excision repair (BER) and nucleotide excision repair (NER), also play an important role in DNA repair in several organisms with the help of a number of glycosylases and polymerases, respectively. In addition, mechanisms such as mutagenic repair or dimer bypass, recombinational repair, cell-cycle checkpoints, apoptosis and certain alternative repair pathways are also operative in various organisms. This review deals with the UV-induced DNA damage and repair in a number of aquatic organisms as well as methods of detecting DNA damage. 相似文献
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Hansch C Verma RP Kurup A Mekapati SB 《Bioorganic & medicinal chemistry letters》2005,15(8):2149-2157
Dopamine receptor blockers have been used for the treatment of schizophrenia for many years. We have developed 22 quantitative structure activity relationships (QSAR) for different sets of compounds to understand chemical-biological interactions governing their activities toward dopamine receptors. 相似文献
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Assembly of the brainstem cochlear nuclear complex is revealed by intersectional and subtractive genetic fate maps 总被引:5,自引:0,他引:5
The cochlear nuclear complex (CN) is the entry point for central auditory processing. Although constituent neurons have been studied physiologically, their embryological origins and molecular profiles remain obscure. Applying intersectional and subtractive genetic fate mapping approaches, we show that this complex develops modularly from genetically separable progenitor populations arrayed as rostrocaudal microdomains within and outside the hindbrain (lower) rhombic lip (LRL). The dorsal CN subdivision, structurally and topographically similar to the cerebellum, arises from microdomains unexpectedly caudal and noncontiguous to cerebellar primordium; ventral CN subdivisions arise from more rostral LRL. Magnocellular regions receive contributions from LRL and coaxial non-lip progenitors; contrastingly, ensheathing granule cells derive principally from LRL. Also LRL-derived and molecularly similar to CN granule cells are precerebellar mossy fiber neurons; surprisingly, these ostensibly intertwined populations have separable origins and adjacent but segregated migratory streams. Together, these findings provide new platforms for investigating the development and evolution of auditory and cerebellar systems. 相似文献