Search results for "ANTITUMOR ACTIVITY"

Synthesis and Antitumor Properties of 2,5-Bis(3'-indolyl) thiophenes: Analogues of Marine Alkaloid Nortopsentin

2007

A series of 11 bis-indolylthiophenes of formula I were obtained by cyclization of bis-indole 1,4-diketones using Lawesson''s reagent. Derivs. I (R = OMe, R1 = SO2Ph), I (R = OMe, R1 = Me), I (R = Cl, R1 = Me), and I (R = OMe, R1 = H) were selected to be evaluated in the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity generally in the micromolar range. The most sensitive cell lines were: CCRF-CEM, MOLT-4, HL60 (TB), and RPMI-8226 of the leukemia subpanel, HT29 and HCC-2998 cell lines of the colon sub-panel, NCI-H522 of the non-small cell lung cancer sub-panel, LOX IMVI of the melanoma sub-panel, and UO-31 of the re…

Synthesis and cytotoxic activity of 3-[2-(1H-indol-3-yl)-1,3-thiazol-4-yl]-1H-pyrrolo[3,2-c]pyridine hydrobromides, analogues of the marine alkaloid …

2021

A new series of thiazole nortopsentin analogues with a 5-azaindole moiety was conveniently synthesized in good to excellent yields by an Hantzsch reaction between thioamides and α-bromoacetyl compounds. The cytotoxic activity of the new derivatives was tested against different human tumor cell lines of the NCI full panel. All tested compounds were active against all of the investigated cell lines showing GI50 values from micro to submicromolar levels. Some of the new analogues exhibited good selectivities against different NCI sub-panels.

Synthesis, spectroscopic characterization and antiproliferative activity of two platinum(II) complexes containing N-donor heterocycles

2014

Abstract Novel mononuclear complexes of Pt(II), cis -[PtCl 2 (DMSO)HL]·2DMSO ( 1 ), where HL = 7-amino-2-(methylthio)[1,2,4]triazolo[1,5- a ]pyrimidine-6-carboxylic acid and Pt(bdt)Cl 2 ( 2 ), where bdt = [2,4-bis(5,6-diphenyl-1,2,4-triazin-3yl)-pyridine] have been synthesized and characterized by elemental analysis, IR and 1 H NMR spectroscopy and X-ray crystallography diffraction analyses. The molecular structure of ( 1 ) shows that Pt(II) ion has a square planar geometry with N(3) bonded heterocycle ligand, two cis chloride anions and S-bonded dimethylsulfoxide. The antiproliferative activity of complexes ( 1 ) and ( 2 ) has been tested in vitro against HepG2 human hepatoma cells and non…

Lack of nucleophilic addition in the isoxazole and pyrazole diketone modified analogs of curcumin; implications for their antitumor and chemosensitiz…

2009

Curcumin (CUR) can be considered as a good lead compound for the design of new anticancer drugs. Further, structure-activity relationship studies may clarify the importance of the redox activities in the antitumor effects of the drug. We have elaborated the alpha,beta-unsaturated 1,3-diketone moiety of CUR into the isoxazole (ISO) and pyrazole (PYR) derivatives. These derivatives should be much less prone to nucleophilic addition than CUR and benzyl mercaptan addition analyses showed that indeed they do not form isolable conjugated products. When compared with CUR, ISO and PYR exhibited increased cell growth inhibitory and pro-apoptotic effects in liver cancer HA22T/VGH cells as well as in …

Antitumoral activity of curcumin: an adjuvant therapeutic strategy

2021

Curcumin, an active substance contained in an Indian spice called turmeric or curcuma, is well known for its anti-inflammatory and antioxidant properties. In recent times, it was taken into account and studied as an antitumoral molecule, by relying on its interference on several biological mechanisms, such as the inhibition of inflammatory mediators, the enhancement of detoxifying enzymes’ action and processes of cell growth and proliferation. Studies show how the high dosage of curcumin in vitro inhibits colorectal tumor cells, pancreatic tumor cells, lung cancer cells and glioblastoma’s cells, interfering in signaling pathways as Wnt/β-catenin, NF-kB and PI3K/Akt and leading to cell cycle…

Bu2Sn(N-acetyl-L-cysteinate) antitumor activity on HepG2 cells

2010

Physiological Effects of Hyperthermia

1987

Hyperthermia as a modality for the treatment of malignant tumors, either alone or in combination with radiation or anticancer drugs, is rapidly becoming a clinical reality. Three different mechanisms of action have provided the rationale for considering the use of hyperthermia as an antitumor agent. At moderate hyperthermia (T=40˚ -42.5˚ C), heat can increase cell killing in a synergistic way following exposure of a tumor to ionizing radiation. This radiosensitization is probably based on, among other things, the inhibited repair of radiation-induced DNA lesions. Elevated tissue temperatures at 40˚ -42.5˚ C also sensitize tumor cells to certain chemotherapeutic drugs, particularly to alkyla…

SYNTHESYS AND ANTITUMOR ACTIVITY OF ISOINDOLO [2,1-A]QUINOXALIN-6-IMINES AND THEIR AZA-ANALOGUES

2014

ISOINDOLO-QUINOXALINE DERIVATIVES HAVING ANTITUMOR ACTIVITY, PROCESS FOR THEIR PRODUCTION AND THEIR USE

2008

New isoindolo[2,1-a]quinoxaline derivatives of general formula (1 ), wherein R represents H or OH and R5 represents H or CN, have been prepared with simple procedures starting from known intermediates and resulted to posses potent in vitro antitumor activity against a panel of about 60 different human tumor cell lines belonging to several kinds of tumors, both hematological and solid. Preparations containing such derivatives as active ingredients are proposed as drugs to be employed in cancer therapy both alone and in combination with other chemotherapeutics.

Synthesis and Antitumor Activity of 3-(2-Phenyl-1,3-thiazol-4-yl)-1H-indoles and 3-(2-Phenyl-1,3-thiazol-4-yl)-1H-7-azaindoles

2011

Given the potent antimicrobial, antiviral, and antitumor activities of many natural products, there is an increasing interest in the synthesis of new molecules based on natural compound scaffolds. Based on a 2,4-bis(3'-indolyl)imidazole skeleton, two new series of phenylthiazolylindoles and phenylthiazolyl-7-azaindoles were obtained by Hantzsch reaction between substituted phenylthioamides and the α-bromoacetyl derivatives. Some azaindole derivatives, tested at the National Cancer Institute against a panel of ∼60 tumor cell lines derived from nine human cancer cell types, showed inhibitory effects against all cell lines investigated at micromolar to nanomolar concentrations. Two of them exh…