Search results for "ANTITUMOR ACTIVITY"

7-Azaindole-fused heterocycles with antitumor activity

2011

New Tripentone Analogs with Antiproliferative Activity

2017

Tripentones represent an interesting class of compounds due to their significant cytotoxicity against different human tumor cells in the submicro-nanomolar range. New tripentone analogs, in which a pyridine moiety replaces the thiophene ring originating the fused azaindole system endowed with anticancer activity viz 8H-thieno[2,3-b]pyrrolizinones, were efficiently synthesized in four steps with fair overall yields (34–57%). All tripentone derivatives were tested in the range of 0.1–100 μM for cytotoxicity against two human tumor cell lines, HCT-116 (human colorectal carcinoma) and MCF-7 (human breast cancer). The most active derivative, with GI50 values of 4.25 µM and 20.73 µM for HCT-116 a…

SYNTHESIS AND ANTITUMOR ACTIVITY OF NEW PYRROLO[2,1-c][1,4]BENZOXAZINES

2009

AZAINDOLO-FUSED HETEROCYCLES: SYNTHESIS AND ANTITUMOR ACTIVITY

2008

Synthesis of the new ring system 6,8-dihydro-5H-pyrrolo[3,4-h]quinazoline

2009

Abstract A convenient synthesis of the pyrrolo[3,4- h ]quinazoline ring system is reported. Our synthetic approach consisted of the annelation of a pyrimidine ring to an isoindole moiety using tetrahydroisoindole-4-ones as building blocks. The antiproliferative activity of the new compounds was investigated and one of them showed antitumor activity against all the 59 tested cell lines at micromolar concentrations (1.46–18.4 μM).

SKRINING FITOKIMIA DAN UJI AKTIVITAS ANTIOKSIDAN DAN ANTITUMOR 20 TUMBUHAN OBAT ASAL KABUPATEN MANOKWARI

2008

<strong><em>Flavanoid, steroid, and terpenoid contents of 20 Manokwari medicinal plants were analyzed.  The antioxidant activity, total phenolic contents and antitumor activity of 20 Manokwari medicinal plants were also evaluated. The result shows that 83% positif to flavanoid test, 59% positif to terpenoid test and only 25% positif steroid. Antioxidant activity and total phenolic contents evaluated using Ferric Thiocianate (FTC) and Folin-Ciocalteu methods respectively. Antioxidant activity and total phenolic contents of medicinal plants were extracted by the traditional method, boiling in water and also in 80% methanol. Twenty plants evaluated in both exstracts have significan…

Synthesis and characterization of complexes of trialkyl- and triarylphosphine gold(I) with thiolated purines and pyrimidines. A class of bifunctional…

1991

Abstract New complexes of the type R 3 PAuL or (R 3 PAu) 2 (μ-L) where R=ethyl or phenyl and L=6-thioguanine, 2, 6- dithioxanthine, 2, 4-dithiouracil and/or dithioerythritol have been prepared. These complexes have been identified by using elemental analysis, 1 H, 13 C and 31 P NMR spectroscopy. The structures have been proposed based on these spectroscopic studies. Sulfur appears to be the binding site in disubstituted complexes of 2, 4-dithiouracil and 1, 4-dithioerythritol, while the phosphine gold( I ) moieties appear to be S and N bonded in 2, 6-dithioxanthine and 6-thioguanine. The potential use of these complexes as antitumor drugs is discussed.

P0311 : Balb/c and C57/Bl6 mice exhibit differences in their susceptibility and anti-tumor response to B16F10 melanoma liver metastasis

2015

Synthesis, chemical characterization and preliminary in vitro antitumor activity evaluation of new ruthenium(II) complexes with sugar derivatives

2011

Abstract Three new complexes of Ru(II), namely [RuCl 2 (Glun-N,O) 2 ]Na 2 ( I ; Glun = glucosaminate), [RuCl 2 (1-Tglu)(EtOH) 2 ]Na ( II ; 1-Tglu = 1-thio-β- d -glucose) and [Ru 2 (EtOH) 6 (AL)Cl 4 ] ( III ; AL = 6′-aminolactose) were prepared from the same Ru(II) precursor, [RuCl 2 (DMSO) 4 ] (DMSO = dimethyl sulfoxide). The characterization of the complexes was carried out by elemental analysis, FT-IR, ES-MS, NMR, EXAFS and DFT calculations. The effectiveness of the complexes on metastatic melanoma A 375 was investigated. The results show that complex II is the most active species.

Pyrrolo[2,1-d][1,2,3,5]tetrazinones deaza analogues of temozolomide with potent antitumor activity

2000

The title compounds, that hold the deaza skeleton of temozolomide, exhibited potent in vitro antiproliferative activity. An evaluation of such a biological activity indicates that the mode of action of these compounds differs from that of temozolomide and is also mechanistically unrelated to that of any known antitumor drug.