Metal-Based Drugs最新文献

{"title":"Synthesis, In vitro Antifungal and Antitumour Activity of Some Triorganotin(IV) N,C,N-Chelates.","authors":"Libor Dostál,&nbsp;Ales Růzicka,&nbsp;Roman Jambor,&nbsp;Vladimír Buchta,&nbsp;Petra Kubanová,&nbsp;Jaroslav Holocek","doi":"10.1155/MBD.2002.91","DOIUrl":"https://doi.org/10.1155/MBD.2002.91","url":null,"abstract":"<p><p>The in vitro antifungal activity of compounds 1-3 ({[(CH3)2NCH2]2C6H3}R2SnX; (where X=Cl, R=n-Bu for 1, X=Br, R=n-Bu for 2 and x=PF6, R=n=Bu for 3)) was estimated with the help of a modified microdilution format of the M27-A guidelines and was compared with in vitro activity of their diphenyltin(IV) analogues 4 and 5 (where X=Br, R=Ph for 4 and X=PF6, R=Ph for 5), and of drugs currently in clinical use (ketoconazole, fluconazole and amphotericin B). It was found that in coordinating solvents the more soluble derivative 2 is less active than the phenyl one (4), and compounds 1 and 3 are even inactive.In this paper, the in vitro antitumour activity of ionic diphenyltin(IV) complexes 4 and 5 against seven tumoural cell lines of human origin is also reported. The preparation and characterization (H1, C13 and Sn119 NMR spectroscopy and electrospray ionization mass spectrometry) of the novel compound 3 is mentioned too.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"9 1-2","pages":"91-6"},"PeriodicalIF":0.0,"publicationDate":"2002-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/MBD.2002.91","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27437509","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthetic, biochemical, antifertility and antiinflammatory aspects of manganese and iron complexes.","authors":"Ashu Chaudhary,&nbsp;Anita Phor,&nbsp;Sanjay Sharma,&nbsp;Anita Gajraj,&nbsp;R V Singh","doi":"10.1155/MBD.2002.97","DOIUrl":"https://doi.org/10.1155/MBD.2002.97","url":null,"abstract":"<p><p>Manganese(II) and iron(II) macrocyclic complexes of polyamide groups have been synthesized by the template codensation of diamines (2,6 diaminopyridine, 1,2 phenylenediamine and 1,3 phenylenediame) and triamine (diethylenetriamine) with phthalic acid in 1:2:2 molar ratios. On the basis of elemental analysis, IR, electronic, magnetic moment, Mössbauer, mass and X-ray spectral studies, octahedral structure has been assigned to [M(N4macn)Cl2] (M = Mn(II) and Fe(II), n = 1 to 4) complexes. The complexes have been screened in vitro against a number of fungi and bacteria to assess their growth inhibiting potential. An attempt has been made to correlate the structural aspects of the compounds with their antiinflammatory and antifertility activities.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"9 1-2","pages":"97-107"},"PeriodicalIF":0.0,"publicationDate":"2002-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/MBD.2002.97","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27437510","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Metal-5-Fluorouracil-histamine complexes: solution, structural, and antitumour studies.","authors":"Sadhna Tyagi,&nbsp;Sukh Mahendra Singh,&nbsp;Sujan Gencaslan,&nbsp;W S Sheldrick,&nbsp;Udai P Singh","doi":"10.1155/MBD.2002.337","DOIUrl":"https://doi.org/10.1155/MBD.2002.337","url":null,"abstract":"<p><p>Solution studies were performed pH-metrically to study the interaction of Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) metal ions with 5-fluorouracil (5FU) and histamine (Hm) separately (binary) and in the presence of each other (ternary) at 25+/-0.1( degrees )C temperature and a constant ionic strength of 0.1 M NaNO(3) in aqueous solution. The ternary complexes have been found to be more stable than the corresponding binary complexes as shown by the positive value of DeltalogK. The species distribution curves have been obtained using the computer programme BEST. On the basis of species distribution results, efforts were also made to prepare some mixed complexes of Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) ions by performing the reaction of their metal nitrates, 5FU and Hm in aqueous ethanol medium at suitable pH. The isolated solid complexes were characterized by different physico-chemical method in order to suggest the possible binding site of the ligands and the structure of the resultant complexes. All these complexes were checked for their antitumour activity by injecting in Dalton's lymphoma (DL) and Sarcoma-180 (S-180) bearing C(3)H/He mice. The results indicate that some complexes have good antitumour activity both in vivo and in vitro.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"8 6","pages":"337-45"},"PeriodicalIF":0.0,"publicationDate":"2002-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/MBD.2002.337","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27440147","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Facile Synthesis of cis-Dichloro-(1,4,7-Triazacyclononane) Platinum(II) and its Screening Against Human Ovarian Cancer (SK-OV-3) and Leukemia (K-562) Cell Lines.","authors":"Robert I Haines,&nbsp;Aleisha M Murnaghan","doi":"10.1155/MBD.2002.61","DOIUrl":"https://doi.org/10.1155/MBD.2002.61","url":null,"abstract":"<p><p>A simple method for the preparation of cis-dichloro(1,4,7-triazacyclononane)platinum(II), cis-Pt(tacn)Cl(2) is presented, together with the results of screening the compound against the K-562 (leukemia) and SK-OV-3 (ovarian) human cancer cell lines. While the compound shows no activity against K-562 cells, there is evidence for some cytotoxicity against SK-OV-3. The compound is much less effective than cisplatin, and its limited solubility restricts the useable concentration range.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"9 1-2","pages":"61-7"},"PeriodicalIF":0.0,"publicationDate":"2002-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/MBD.2002.61","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27437506","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis and cytotoxicity of silicon containing pyridine and quinoline sulfides.","authors":"Edmunds Lukevics,&nbsp;Edgars Abele,&nbsp;Pavel Arsenyan,&nbsp;Ramona Abele,&nbsp;Kira Rubina,&nbsp;Irina Shestakova,&nbsp;Ilona Domracheva,&nbsp;Violetta Vologdina","doi":"10.1155/MBD.2002.45","DOIUrl":"https://doi.org/10.1155/MBD.2002.45","url":null,"abstract":"<p><p>Silicon containing pyridine and quinoline sulfides have been prepared using phase transfer catalytic system thiol/alkyl halide / solid KOH/18-crown-6 / toluene. The target S-ethers were isolated in yields up to 81%. The cytotoxicity of the synthesized compounds was studied. Among pyridine sulfides S-[3-(1-methyl- 1-silacyclohexyl)propyl] derivatives 5e and 6e exhibit the highest cytotoxicity. Aliphatic silicon derivatives were considerably less active. 8-[(Trimethylsilylmethyl)thio]quinoline (8a) exhibits the highest activity among quinoline sulfides.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"9 1-2","pages":"45-51"},"PeriodicalIF":0.0,"publicationDate":"2002-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/MBD.2002.45","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27437620","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Cerebroprotective Effects of Dimeric Copper(II) Bis(o-acetoxybenzoate) on Ischemia-reperfusion Injury in Gerbils.","authors":"Ling Li,&nbsp;Zhiqiang Shen,&nbsp;Weimin Yang,&nbsp;Wanling Wu,&nbsp;Weiping Liu,&nbsp;Zhihe Chen","doi":"10.1155/MBD.2002.253","DOIUrl":"https://doi.org/10.1155/MBD.2002.253","url":null,"abstract":"<p><p>The cerebroprotective effects of copper aspirinate [dimeric copper(II) bis(o-acetoxybenzoate)] were investigated in gerbils subjected to 10-min global cerebral ischemia followed b 60-min reperfusion. The results showed that intragastric copper aspirinate (7.5, 15.0 and 30.0 mg Kg(-1)) markedly promoted the recovery of the electroencephalogram amplitude, attenuated the increase of lipid peroxide content and the decrease of superoxide dismutase activity in the cortex during ischemia-reperfusion injury. It suggested that copper aspirinate possesses potential neuroprotective properties, the mechanism of which might be related to an increase of the activity of endogenous superoxide dismutase.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"8 5","pages":"253-6"},"PeriodicalIF":0.0,"publicationDate":"2002-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/MBD.2002.253","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27437889","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Efficacy of organophosphorus derivatives containing chalcones/chalcone semicarbazones against fungal pathogens of sugarcane.","authors":"S K Sengupta,&nbsp;O P Pandey,&nbsp;G P Rao,&nbsp;Priyanka Singh","doi":"10.1155/MBD.2002.293","DOIUrl":"https://doi.org/10.1155/MBD.2002.293","url":null,"abstract":"<p><p>Ten newly synthesized organophosphorus derivatives containing substituted chalcones and substituted chalcone semicarbazones were tested for their antifungal efficacy against Colletotrichum falcatum, Fusarium oxysporum, Curvularia pallescens (all sugarcane pathogens). The O,O-diethylphosphate derivatives containing 2-chlorochalcone and 2-chlorochalcone semicarbazone exhibited 70-85% mycelial inhibition against all the test fungi at 1000 ppm. The screening results were correlated with structural features of the tested compounds.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"8 5","pages":"293-302"},"PeriodicalIF":0.0,"publicationDate":"2002-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/MBD.2002.293","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27437896","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Silacyclic derivatives of heteroaromatic sulfides as selective cholesterol level lowering and vasodilating agents.","authors":"Edgars Abele,&nbsp;Kira Rubina,&nbsp;Ramona Abele,&nbsp;Olegs Dzenitis,&nbsp;Pavel Arsenyan,&nbsp;Juris Popelis,&nbsp;Maris Veveris,&nbsp;Dainuvite Meirena,&nbsp;Edmunds Lukevics","doi":"10.1155/MBD.2002.307","DOIUrl":"https://doi.org/10.1155/MBD.2002.307","url":null,"abstract":"<p><p>Silacyclic derivatives of heteroaromatic sulfides have been prepared by using phase transfer catalytic (PTC) system thiol / silacyclopropyl iodide / solid K(2)CO(3) / 18-crown-6 / toluene. The target sulfides were isolated in yields up to 70 %. The S-derivatives of N-methylimidazolyl, benzoxazolyl and 1,3,4-triazolyl thiols selectively lowered the low density lipoprotein (LDL) level in mice with the high cholesterol diet in nutrition.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"8 6","pages":"307-13"},"PeriodicalIF":0.0,"publicationDate":"2002-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/MBD.2002.307","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27437898","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Biologically Active Co(II) and Ni(II) Complexes of N-(2-Thienylmethylene)-2-Aminothiadiazole.","authors":"Zahid H Chohan","doi":"10.1155/MBD.2002.323","DOIUrl":"https://doi.org/10.1155/MBD.2002.323","url":null,"abstract":"<p><p>Co(II) and Ni(II) complexes Schiff base, N-(2-thienylmethylene)-2-aminothiadiazole have been prepared and characterized by their physical, spectral and analytical data. The title Schiff-base acts as NNS donor tridentate during the complexation reaction with these metal ions having a composition, [M(L)(2)]X(n) where M=Co(II) or Ni(II), L=, X=NO(3) (-), SO(4) (2-), C(2)O(4) (2-) or CH(3)CO(2) (-) and n=1 or 2 and show an octahedral geometry. In order to evaluate the effect anions upon chelation, the Schiff-base and its new complexes have been screened for their antibacterial activity against bacterial strains e.g., Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"8 6","pages":"323-7"},"PeriodicalIF":0.0,"publicationDate":"2002-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/MBD.2002.323","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27437900","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis and cytotoxicity of cyanoborane adducts of n6-benzoyladenine and 6-triphenylphosphonylpurine.","authors":"Tanya C Scarlett,&nbsp;Richard W Durham,&nbsp;Iris H Hall,&nbsp;Richard J Crosswicks,&nbsp;Joshua D Berkowitz,&nbsp;Bruce S Burnham","doi":"10.1155/MBD.2002.19","DOIUrl":"https://doi.org/10.1155/MBD.2002.19","url":null,"abstract":"<p><p>N6-Benzoyladenine-cyanoborane (2), and 6-triphenylphosphonylpurine-cyanoborane (3) were selected for investigation of cytotoxicity in murine and human tumor cell lines, effects on human HL-60 leukemic metabolism and DNA strand scission to determine the feasibility of these compounds as clinical antineoplastic agents. Compounds 2 and 3 both showed effective cytotoxicity based on ED(50) values less than 4 mug/ml for L1210, P388, HL-60, Tmolt(3), HUT-78, HeLa-S(3) uterine, ileum HCT-8, and liver Hepe-2. Compound 2 had activity against ovary 1-A9, while compound 3 was only active against prostate PL and glioma UM. Neither compound was active against the growth of lung 549, breast MCF-7, osteosarcoma HSO, melanoma SK2, KB nasopharynx, and THP-1 acute monocytic leukemia. In mode of action studies in human leukemia HL-60 cells, both compounds demonstrated inhibition of DNA and protein syntheses after 60 min at 100 muM. These compounds inhibited RNA synthesis to a lesser extent. The utilization of the DNA template was suppressed by the compounds as determined by inhibition of the activities of DNA polymerase alpha, m-RNA polymerase, r-RNA polymerase and t-RNA polymerase, which would cause adequate inhibition of the synthesis of both DNA and RNA. Both compounds markedly inhibited dihydrofolate reductase activity, especially in compound 2. The compounds appeared to have caused cross-linking of the DNA strands after 24 hr at 100 muM in HL-60 cells, which was consistent with the observed increased in ct-DNA viscosity after 24 hr at 100 muM. The compounds had no inhibitory effects on DNA topoisomerase I and II activities or DNA-protein linked breaks. Neither compound interacted with the DNA molecule itself through alkylation of the nucleotide bases nor caused DNA interculation between base pairs. Overall, these antineoplastic agents caused reduction of DNA and protein replication, which would lead to killing of cancer cells.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"9 1-2","pages":"19-32"},"PeriodicalIF":0.0,"publicationDate":"2002-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/MBD.2002.19","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27437618","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}