共查询到20条相似文献,搜索用时 15 毫秒
1.
Cosimo G. Fortuna Vincenza Barresi Giuseppe Musumarra 《Bioorganic & medicinal chemistry》2010,18(12):4516-4523
A modeling approach based on physico-chemical and pharmacokinetic properties, called Volsurf+, was used to design new trans 2-(thiophen-2-yl)vinyl heteroaromatic iodides with antiproliferative activity. The synthesis and in vitro antitumor tests on two cell lines (MCF-7 and LNCap) confirmed Volsurf predicted activity values. An Almond model, derived to have an overall structural insight on the above compounds, supported the validity of Volsurf and provided guidelines for the synthesis of new compounds. 相似文献
2.
Dong Jin Kim Kyung Jae Seo Kyung Seok Lee Kye Jung Shin Kyung Ho Yoo Dong Chan Kim Sang Woo Park 《Bioorganic & medicinal chemistry letters》2000,10(24):1-2802
A new series of 1β-methylcarbapenems 1a–i bearing isoxazoloethenyl groups on the pyrrolidine ring has been prepared and evaluated for in vitro antibacterial activity and stability to DHP-I. Most compounds showed excellent antibacterial activity and high stability to DHP-I superior to that of meropenem. Of these new carbapenems, 1a,b,h exhibited the best combination of antibacterial activity and DHP-I stability. 相似文献
3.
研究了H2 O2 和蛋白水解酶在小麦 (TriticumaestivumL .cv.Yanmai15 8)叶片老化过程中的关系。小麦叶片老化期间 ,H2 O2 含量高的叶片中内肽酶活力也高。老化后期 ,内源H2 O2 迅速累积 ,内肽酶活力迅速上升 ;通过内肽酶同工酶电泳可检测到新增一种活力较强的内肽酶。用外源H2 O2 处理全展旗叶的内肽酶粗提液 ,随着H2 O2 浓度的升高 ,内肽酶活力先上升后下降。 相似文献
4.
Kim DJ Seo KJ Lee KS Shin KJ Yoo KH Kim DC Park SW 《Bioorganic & medicinal chemistry letters》2000,10(24):2799-2802
A new series of 1beta-methylcarbapenems 1a-i bearing isoxazoloethenyl groups on the pyrrolidine ring has been prepared and evaluated for in vitro antibacterial activity and stability to DHP-I. Most compounds showed excellent antibacterial activity and high stability to DHP-I superior to that of meropenem. Of these new carbapenems, 1a,b,h exhibited the best combination of antibacterial activity and DHP-I stability. 相似文献
5.
Narender P Srinivas U Gangadasu B Biswas S Rao VJ 《Bioorganic & medicinal chemistry letters》2005,15(24):5378-5381
New Baylis–Hillman adducts are synthesized based on substituted 2-chloronicotinaldehydes and screened for their in vitro anti-malarial activity against chloroquine sensitive and chloroquine resistant Plasmodium falciparum. Out of the six new compounds synthesized and screened, 2b, 2c and 2d compounds showed substantial anti-malarial activity. 相似文献
6.
The relationship between hydrogen peroxide (H2O2) and endopeptidase(EP) in wheat (Triticum aestivum L. cv. Yanmai 158) leaves was studied during natural and artificial aging. Rapid accumulation of endogenous H2O2 and marked increase of EP activity were observed during the later phase of aging. A new EP isozyme with higher activity was detected by electrophoresis on polyacrylamide gels containing denatured heamoglobin. With the increase of exogenous H2O2, the activity of EP increased at first and then decreased. 相似文献
7.
Han SY Choi JW Yang J Chae CH Lee J Jung H Lee K Ha JD Kim HR Cho SY 《Bioorganic & medicinal chemistry letters》2012,22(8):2837-2842
A series of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2-yl)-1H-quinolin-2-ones have been identified as a new class of VEGFR-2 kinase inhibitors. A variety of (4,5,6,7-tetrahydro-imidazo[5,4-c]pyridin-2-yl)-acetic acid ethyl esters were synthesized, and their VEGFR-2 inhibitory activity was evaluated. Described herein are the preparation of the series and the effects of the compounds on VEGFR-2 kinase activity. 相似文献
8.
3-nitro-2H-chromenes and derivatives are compounds with diverse biological activity, among them, new 2-glyco-3-nitro-2H-chromenes have been prepared by one-pot oxa-Michael-Henry-dehydration reactions between carbohydrate-derived nitroalkenes and several salicylaldehydes, using a minimal amount of solvent and DBU as catalyst. The antiproliferative activity of these new compounds has been evaluated against a panel of six human solid tumor cell lines, and compared to pharmacological reference compounds, finding that their activities are in the low micromolar range and that some of them are more effective than the standards. 相似文献
9.
10.
O'Leary KA de Pascual-Tereasa S Needs PW Bao YP O'Brien NM Williamson G 《Mutation research》2004,551(1-2):245-254
11.
Suhara Y Murakami A Kamao M Mimatsu S Nakagawa K Tsugawa N Okano T 《Bioorganic & medicinal chemistry letters》2007,17(6):1622-1625
Novel omega-oxygenated vitamin K2 analogues, which are candidates for metabolites of vitamin K2 homologues, were efficiently synthesized and their apoptosis-inducing activity was evaluated. We revealed that some of those analogues were biologically active and the side-chain part played an important role in apoptosis-inducing activity. Our results can provide useful information to develop the structure-activity relationship of vitamin K2 analogues for new drugs based on vitamin K. 相似文献
12.
Paul V. Bernhardt Gregory J. Wilson Philip C. Sharpe Danuta S. Kalinowski Des R. Richardson 《Journal of biological inorganic chemistry》2008,13(1):107-119
2-Pyridinecarbaldehyde isonicotinoyl hydrazone (HPCIH) and di-2-pyridylketone isonicotinoyl hydrazone (HPKIH) are two Fe chelators
with contrasting biological behavior. HPCIH is a well-tolerated Fe chelator with limited antiproliferative activity that has
potential applications in the treatment of Fe-overload disease. In contrast, the structurally related HPKIH ligand possesses
significant antiproliferative activity against cancer cells. The current work has focused on understanding the mechanisms
of the Fe mobilization and antiproliferative activity of these hydrazone chelators by synthesizing new analogs (based on 2-acetylpyridine
and 2-benzoylpyridine) that resemble both series and examining their Fe coordination and redox chemistry. The Fe mobilization
activity of these compounds is strongly dependent on the hydrophobicity and solution isomeric form of the hydrazone (E or Z). Also, the antiproliferative activity of the hydrazone ligands was shown to be influenced by the redox properties of the
Fe complexes. This indicated that toxic Fenton-derived free radicals are important for the antiproliferative activity for
some hydrazone chelators. In fact, we show that any substitution of the H atom present at the imine C atom of the parent HPCIH
analogs leads to an increase in antiproliferative efficacy owing to an increase in redox activity. These substituents may
deactivate the imine R–C=N–Fe (R is Me, Ph, pyridyl) bond relative to when a H atom is present at this position preventing
nucleophilic attack of hydroxide anion, leading to a reversible redox couple. This investigation describes novel structure–activity
relationships of aroylhydrazone chelators that will be useful in designing new ligands or fine-tuning the activity of others.
Electronic supplementary material The online version of this article (doi:) contains supplementary material, which is available to authorized users. 相似文献
13.
14.
Nikiforov AK Volokh OA Lobovikova OA Diatlov IA Zhulidov IM 《Zhurnal mikrobiologii, epidemiologii, i immunobiologii》2007,(1):72-74
Technology of manufacturing of new anti-rabies immunoglobulin preparation based on F(ab')2 fragments has been developed. This preparation is characterized by low reactogenicity, increased virus-neutralizing activity and stability. 相似文献
15.
Hg^2+对金银莲花根和叶片的伤害 总被引:6,自引:0,他引:6
研究了汞离子胁迫下金银莲花〔Nymphoidesindica(L.)Kuntze〕根受害情况、根部过氧化物酶活性和新叶叶绿素含量的变化。根部受害程度随汞离子浓度升高和处理时间的延长而加重。低浓度Hg2+短时间处理后根过氧化物酶活性升高,而高浓度Hg2+长时间处理后根过氧化物酶活性下降,且随着Hg2+浓度的升高或处理时间的延长过氧化物酶活性均呈下降趋势。新叶叶绿素含量对Hg2+胁迫的反应与根过氧化物酶活性的变化相似。 相似文献
16.
A series of new 2-(2-aminopyrimidin-4-yl)phenol derivatives were synthesized as potential antitumor compounds. Substitution with pyrrolidine-3,4-diol at the 4-position of phenol provided potent inhibitory activity against CDK1 and CDK2. X-ray crystal structural studies were performed to account for the effect of the substituent on both the enzymatic and cell growth inhibitory activities. 相似文献
17.
R B Banerjee R Bhadra A G Datta 《Biochemical and biophysical research communications》1983,115(2):506-511
Alanine-2-oxoglutarate aminotransferase activity in mouse liver is stimulated by the intravenous injection of glucagon. The stimulation is abolished by pretreatment with actinomycin D indicating that the increased activity is probably due to new enzyme formation. Administration of dibutyryl cyclic AMP, isoproterenol, an activator of adenyl cyclase and theophylline, an inhibitor of phosphodiesterase also increases the enzyme activity suggesting the involvement of cyclic AMP in glucagon-mediated increase of enzyme activity. 相似文献
18.
Harrison LE Wang QM Studzinski GP 《Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.)》1999,222(2):150-156
Butyrate, a short-chain fatty acid, has been reported to inhibit proliferation and stimulate differentiation in multiple cancer cell lines. Whereas the effects of butyrate on cellular differentiation are well documented, the relationship between butyrate-induced differentiation and its effect on cell cycle traverse is less well understood. The purpose of this study was to investigate the effects of butyrate on the regulatory proteins of the G2/M traverse in the Caco-2 colon cancer cell model. We demonstrated that the inhibition of proliferation and increased cellular differentiation after treatment of Caco-2 cells with butyrate were associated with a significant G2/M cell cycle block. Although protein levels of the major G2/M regulatory protein, p34cdc2, were unchanged, a decrease in p34cdc2 activity was noted. Despite this decrease in activity, the inhibitory tyrosine phosphorylation of p34cdc2 was decreased, suggesting that other factors are responsible for the decreased kinase activity. The reduced activity of p34cdc2 provides a possible mechanism for the accumulation of Caco-2 cells in the G2/M cell cycle compartment following exposure to butyrate. This cell system provides a new model for studies of G2/M cell cycle perturbations. 相似文献
19.
Zhi Jie Shan Hong Lin Zhai Xiao Yan Huang Li Na Li Xiao Yun Zhang 《Bioorganic & medicinal chemistry letters》2013,23(19):5339-5350
Aggrecanases-2 is a very important potential drug target for the treatment of osteoarthritis. In this study, a series of known aggrecanases-2 inhibitors was analyzed by the technologies of three-dimensional quantitative structure–activity relationships (3D-QSAR) and molecular docking. Two 3D-QSAR models, which based on comparative molecular field analysis (CoMFA) and comparative molecular similarity analysis (CoMSIA) methods, were established. Molecular docking was employed to explore the details of the interaction between inhibitors and aggrecanases-2 protein. According to the analyses for these models, several new potential inhibitors with higher activity predicted were designed, and were supported by the simulation of molecular docking. This work propose the fast and effective approach to design and prediction for new potential inhibitors, and the study of the interaction mechanism provide a better understanding for the inhibitors binding into the target protein, which will be useful for the structure-based drug design and modifications. 相似文献
20.
Fibroblast growth factor-2 总被引:23,自引:0,他引:23
Fibroblast growth factor-2 (FGF-2) is a member of a large family of proteins that bind heparin and heparan sulfate and modulate the function of a wide range of cell types. FGF-2 stimulates the growth and development of new blood vessels (angiogenesis) that contribute to the pathogenesis of several diseases (i.e. cancer, atherosclerosis), normal wound healing and tissue development. FGF-2 contains a number of basic residues (pI 9.6) and consists of 12 anti-parallel beta-sheets organized into a trigonal pyrimidal structure. FGF-2 binds to four cell surface receptors expressed as a number of splice variants. Many of the biological activities of FGF-2 have been found to depend on its receptor's intrinsic tyrosine kinase activity and second messengers such as the mitogen activated protein kinases. However, considerable evidence suggest that intracellular FGF-2 might have a direct biological role particularly within the nucleus. In addition, heparan sulfate proteoglycans have been demonstrated to enhance and inhibit FGF-2 activity. The possibility that FGF-2 activity can be manipulated through alterations in heparan sulfate-binding is currently being exploited in the development of clinical applications aimed at modulating either endogenous or administered FGF-2 activity. 相似文献