Potential Antitumor Agents (potential + antitumor_agent)

Distribution by Scientific Domains
Distribution within Chemistry

Selected Abstracts

Synthesis of Polyamines from Ethylenediamine and Their Platinum(II) Complexes, Potential Antitumor Agents

Mara Rubia Costa Couri
Abstract This work describes the synthesis and characterization of five new amine ligands and also the preparation and characterization of their respective platinum(II) complexes by reaction with K2PtCl4 in water. These ligands were obtained by treatment of different halides or epoxides with ethylenediamine. Cytotoxic activity and cellular accumulation of three complexes were investigated in a human small-cell lung carcinoma cell line and its cisplatin resistant subline. The introduction of a spacer (cycle) between the two platinum atoms leads to a significant decrease in cytotoxic activity. At equitoxic doses, the intracellular platinum concentrations found for compounds 12 and 15 were significantly higher than those found for the reference compounds, cisplatin, carboplatin, or compound 9. This fact suggests that the formation of adducts between compounds 12 and 15 and the putative pharmacological target, DNA, is less favored. If these compounds bind more slowly to DNA, interaction with other intracellular ligands such as sulfur-containing molecules will become relevant and it may be the reason for the elevated intracellular platinum concentrations. ( Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2006) [source]

Platinum and Palladium-triazole Complexes as Highly Potential Antitumor Agents

Najim A. Al-Masoudi
Abstract The palladium complexes [(dppe)Pd(L)2PdCl2], [(dppe)Pd(L)2PtCl2], [(dppp)Pd(L)2PdCl2], [(dppm) Pd(L)2NiCl2], and [(dppm)Pd(L)2SnCl4] 15,19 were prepared. The antiproliferative activity of the newly synthesized complexes as well as their previously prepared analogues 3,14 and 20,26 were screened against a large panel of human cancer cell lines derived from haematological CD4+ human T-cells containing an integrated HTLV-1 genome (MT-4). The complex 12a, b exhibited remarkable antiproliferative activity against MT-4, CD4+ human acute T-lymphoblastic leukemia (CCRF-CEM), human splenic B-lymphoblastoid cells (WIL-2NS), human acute B-lymphoblastic leukemia (CCRF-SB), skin melanoma (SK-MEL-28), and prostate carcinoma (DU145) cell lines (CC50 = 0.5 ,M, 0.4 0.05 ,M, 0.6 0.05 ,M, 0.4 0.1 ,M, and 0.8 0.2 ,M, respectively), meanwhile, 9a, b, 14a, b, and 23 showed significant activity against the CCRF-SB cell lines (CC50 = 0.6 0.06 ,M, 0.7 0.05 ,M, 0.6 0.05 ,M, and 0.8 0.15 ,M, respectively). Further, 19 exhibited activity against the CCRF-CEM cell line (CC50 = 0.4 0.05 ,M). [source]

ChemInform Abstract: Synthesis of (3-Amino-7-chloro-8-methyl-1,1-dioxo-4H-1,5,2-benzo [f]dithiazepin-4-ylidene)acetic Acid Derivatives as Potential Antitumor Agents.

CHEMINFORM, Issue 21 2008
Z. Brzozowski
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]

Synthesis and Biological Evaluation of a Novel Phenyl Substituted Sydnone Series (VII) as Potential Antitumor Agents.

CHEMINFORM, Issue 47 2003
Christopher S. Dunkley
No abstract is available for this article. [source]

Novel 3-benzoyl-2-piperazinylquinoxaline derivatives as potential antitumor agents

Sandra Piras
A series of new benzoylquinoxaline derivatives (7-26) was synthesized and evaluated for antitumor activity against a panel of 60 human cell lines at the NCI of Bethesda. Among the compounds which have passed the preliminary screening, compound 23 exhibited the best profile and growth inhibition activity at 100 - 10 ,M. The compounds were then tested towards a folate-dependent enzymes bio-library including Thymidylate synthases enzymes and human Dihydrofolate reductase at 10 ,M. The most of compounds exhibited a moderate inhibitory activity towards all or some of the enzymes tested with detectable inhibition constants (Ki) values in the range of 0.6-70 ,M. Compounds 21, 23, 24 showed Ki in the range of 10-38 ,M against both hDHFR and hTS. [source]

In vitro antiproliferative effect of six Salvia species on human tumor cell lines

Giovina Fiore
Abstract This study was designed to examine the in vitro antiproliferative activity of the methanol crude extracts of six Salvia species: Salvia dominica L. leaves, Salvia lanigera Desf. aerial parts, Salvia menthaefolia Ten. roots, Salvia palaestina Benth. aerial parts, Salvia sclarea L. roots and Salvia spinosa L. aerial parts. Extracts were screened for their possible antitumoral activity by MTT test on nine human cancer cell lines: glioblastoma (DBTRG-05MG, T98G, U-87MG), colorectal adenocarcinoma (WiDr and HT-29), prostate adenocarcinoma (MDA Pca2b), choriocarcinoma (JEG-3), endometrium adenocarcinoma (HEC-1A) and B lymphoblast (CIR). IC50 values were determined for only five extracts and ranged from 90 to 400 mg/mL approximately. Salvia menthaefolia extract exhibited marked antiproliferative activity against all tumor cell lines showing lower IC50 values, while S. spinosa, S. sclarea and S. dominica extracts showed a degree cytotoxic activity dependent on the cell line type. Finally S. palaestina extract revealed a moderate antiproliferative effect only against three cell lines. Salvia lanigera extract displayed toxic activity at all concentrations tested. The results strengthen the evidence that the genus Salvia could be considered a natural resource of potential antitumor agents. Copyright 2006 John Wiley & Sons, Ltd. [source]

Synthesis and In-Vitro Cytotoxicity Evaluation of Novel Naphtindolizinedione Derivatives, Part II: Improved Activity for Aza-Analogues

Andrea Defant
Abstract Our previous investigation on potential antitumor agents now got enriched by the evaluation of in-vitro activity against a full panel of NCI cancer cell lines for five new compounds. The concurrent presence in the molecular structure of a nitrogen atom in the aromatic system and a N,N -dimethylaminoethyl amide chain play a decisive role to enhance cytotoxicity. The N,N -anti compound 14 shows a higher activity than its N,N -syn isomer, exhibiting the best selective inhibition against the melanoma MALME-3M cell line, with a GI50 -value (= 30 nM) corresponding to a 330-fold increase in activity compared to the corresponding deaza-analogue. Compound 14 is efficiently synthesized by aminolysis of the ester obtained as a single regio-isomer by an one-pot three-component procedure involving metal-assisted cyclization under microwave irradiation conditions. [source]

Structure-Based Design, Synthesis, and Evaluation of 2,-(2-Hydroxyethyl)-2,-deoxyadenosine and the 5,-Diphosphate Derivative as Ribonucleotide Reductase Inhibitors

CHEMMEDCHEM, Issue 10 2009
Dianqing Sun Dr.
Abstract Analysis of the recently solved X-ray crystal structures of Saccharomyces cerevisiae ribonucleotide reductase,I (ScRnr1) in complex with effectors and substrates led to the discovery of a conserved water molecule located at the active site that interacted with the 2,-hydroxy group of the nucleoside ribose. In this study 2,-(2-hydroxyethyl)-2,-deoxyadenosine 1 and the 5,-diphosphate derivative 2 were designed and synthesized to see if the conserved water molecule could be displaced by a hydroxymethylene group, to generate novel RNR inhibitors as potential antitumor agents. Herein we report the synthesis of analogues 1 and 2, and the co-crystal structure of adenosine diphosphate analogue 2 bound to ScRnr1, which shows the conserved water molecule is displaced as hypothesized. [source]