Search results for "Antitumor Activity"
showing 10 items of 85 documents
A Facile Synthesis of Deaza-Analogues of the Bisindole Marine Alkaloid Topsentin
2013
A series of substituted ethyl 1-[(tert-butoxycarbonyl)amino]-2-methyl-5- (1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)carbonyl]-1H-pyrrole-3-carboxylates were prepared in excellent yields (82-98%) by one-pot reactions between β-dicarbonyl compounds 12a-e and 1,2-diaza-1,3-diene (DD) 13. Derivatives 10a,c-e, deazaanalogues of the bis-indole alkaloid topsentin, screened by the National Cancer Institute (Bethesda, MD, USA) in the in vitro one dose primary anticancer assay against a panel of about 60 human tumor cell lines, showed no significant activity, with the exception of compound 9e, which showed moderate activity against the HOP-92 cell line of the non small cell lung cancer sub-p…
Lead optimization through VLAK protocol: New annelated pyrrolo-pyrimidine derivatives as antitumor agents
2012
Abstract The chemometric protocol VLAK was applied to predict improvement of the biological activity of pyrrolo-pyrimidine derivatives as anticancer agents, by using the NCI ACAM Database as depository of antitumor drugs with a known mechanism of action. Among the selected compounds two of these showed a good increase in the antitumor activity. These new pyrrolo-pyrimidine compounds were demonstrated effective against the full panels of NCI DTP tumour human cell lines. The derivative 8-[3-(piperidino)propyl]-4,10-dimethyl-9-phenyl-6-(methylsulfanyl)-3,4-dihydropyrimido[1,2-c]pyrrolo[3,2-e]pyrimidin-2(8H)-one reveled efficacious against the leukemia subpanel, in particular the RPMI cell line…
Synthesis and structures of some diorganotin bis(hydroxamate)s
1994
Analysis of literature data on the antitumor activity of organotin compounds reveals that R2SnX2 and their complexes containing SnO, SnN or SnS bonds often exhibit biological activity, especially if such bonds are formed by means of intramolecular coordination. Furthermore, a wide range of biological activities, from fungicidal, bactericidal and antiseptic to psychotropic and antitumor, is found to be characteristic for some organic hydroxamic acids (N-acylhydroxylamines). From this point of view the diorgantion bis-hydroxamates in this paper are of particular interest as potential biologically active antitumor drugs. Di-n-butyltin bis(N-methyl-N-p-bromobenzoylhydroxylamine) is being screen…
Anti-tumor activity of two binuclear gold(I) complexes with bridging dithiolate ligands
1986
Abstract Two new binuclear complexes of gold with bridging dithiolate ligands were synthesized and characterized: (o3PAu)2(μ-DTE) and (Et3PAu)2(μ-DMTA); H2DTE=dithioerylthritol and H2DMTA=2,5-dimer- capto-1-thia-3,4-diazole. These compounds and three gold compounds with antiarthritic activity (gold sodium thiomalate, gold thioglucose and Et3PAuCl) were tested for antitumor activity using the Ehrlich- Ascites tumor cell in mice. Only (o3PAu)e(μ-DTE) showed significant activity.
Mono- and polynuclear complexes of Pt(II) with polypyridyl ligands. Synthesis, spectroscopic and structural characterization and cytotoxic activity.
2007
Abstract An array of poly- and mononuclear complexes of Pt(II) with polypyridyl ligands is reported. The framework complexes [(PtCl 2 ) 2 (bpp) 2 (μ-PtCl 2 )](H 2 O) 2 [bpp = 2,3-bis(2-pyridyl)pyrazine], [PtCl 2 (μ-tptz)PtClNCPh]Cl [tptz = 2,4,6-tris(2-pyridyl)-1,3,5-triazine], and mononuclear PtCl 2 (NH 2 dpt) [NH 2 dpt = 4-amino-3,5-bis(2-pyridyl)-1,2,4-triazole] have been prepared and structurally characterized. Both neutral and ionic complexes are present, with bifunctional and monofunctional Pt(II) moieties, whose size and shape enable them to behave as novel scaffolds for DNA binding. Pt(II) complexes were tested for their biological activity. Cell viability assay and flow cytometric …
Screening of fractions from marine sponges and other invertebrates to identify new lead compounds with anti-tumor activity in lymphoma models
2020
Diffuse large B-cell lymphoma (DLBCL) is the commonest type of lymphomas, accounting for 30%-40% of new cases each year. Despite the big improvements achieved in the treatment, still 25–40% of patients still succumb due to refractory or relapsed disease. This highlights the need of new drugs for this cancer. The marine environment has recently been recognized as a source of anti-cancer compounds, as demonstrated by different marine drugs approved by different regulatory agencies (trabectedin, cytarabine, eribulin, plitidepsin) or as components of antibody drug conjugates for lymphoma patients (monomethyl auristatin E in polatuzumab vedotin and brentuximab vedotin). Here, we present a large …
Synthesis, structural characterization, anti-proliferative and antimicrobial activity of binuclear and mononuclear Pt(II) complexes with perfluoroalk…
2018
Abstract In this paper we report the synthesis of four Pt(II) complexes with 5-perfluoroalkyl-1,2,4-oxadiazolyl-pyridine and 3-perfluoroalkyl-1-methyl-1,2,4-triazolyl-pyridine ligands. Two binuclear complexes [PtCl(pfibap)2](µ-Cl)2 (1), [Pt2(µ-Cl)2(pfioap)4]Cl2 (2), and two mononuclear [PtCl2(pfptp)] (3), [PtCl2(pfhtp)2] (4), were synthesized with the ligands: 2-(5-perfluoropropyl)-1,2,4-oxadiazole-3yl)-pyridine (pfpop), 2-(5-perfluoroheptyl-1,2,4-oxadiazole-3yl)-pyridine (pfhop), 2-(3-perfluoropropyl-1-methyl-1,2,4-triazole-5yl)-pyridine (pfptp), 2-(3-perfluoroheptyl-1-methyl-1,2,4-triazole-5yl)-pyridine (pfhtp), and were structurally characterized. All complexes were tested in vitro on th…
The oral KIF11 inhibitor 4SC‐205 exhibits antitumor activity and potentiates standard and targeted therapies in primary and metastatic neuroblastoma …
2021
Inhibidor de KIF11; Terapias dirigidas; Metástasis Inhibidor de KIF11; Teràpies dirigides; Metàstasi KIF11 inhibitor; Targeted therapies; Metastasis In summary, our study provides a rationale for the future therapeutic integration in clinical trials of 4SC-205, an structurally distinct oral KIF11 inhibitor that shows potent antitumor activity in multiple preclinical neuroblastoma models and sensitizes neuroblastoma cells to standard chemotherapy and specific neuroblastoma-targeted therapies. The financial support for this research was provided by Instituto de Salud Calos III (PI20/00530 to Miguel F. Segura; PI20/01107 to Rosa Noguera; PI17/02248 and CPII18/00027 to Anna Santamaria; PI19/013…
3,5-bis(3'-indolyl)pyrazoles, analogues of marine alkaloid nortopsentin: synthesis and antitumor properties.
2007
A series of 10 bis-indolylpyrazoles of type 9, 10 were obtained by cyclization of diketones 8 using hydrazine monohydrate or methylhydrazine in refluxing acetic acid/THF. Derivatives 9a,c,d were selected, by the National Cancer Institute (NCI, Bethesda, USA), to be evaluated against the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity in the micromolar range. In particular, 9d, the most active compound was effective against all the tested cell lines with a GI(50) mean value of 3.23 microM; TGI and LC(50) values were 14.5 and 58.9 microM having positive response on 91% and 41% of the tested cell lines, respectively.