Search results for "Zole"
showing 10 items of 2482 documents
SYNTHESIS AND SAR STUDIES OF NEW 3-METHYL-5-(5-PROPYL-1H-1-R'-3-PYRAZOLYL)-1H-1-R-4-NITROSOPYRAZOLES AS ANTIMICOTIC AGENTS.
2013
Solvent-dependent hypsochromic shift in the imidazole based complex [Cu(µ2-SO4)(Im)4] and ameliorative effects on breast cancer-induced bone metastas…
2023
A sulfate-bridged complex [Cu(µ2-SO4)(Im)4] (1) was prepared and structurally characterized, where Im: imidazole. The X-ray structure analysis reveals that 1 crystallizes in the monoclinic system with space group C2/c. The octahedral coordination around the metal center is made up of four distinct imine nitrogen atoms in the equatorial plane, and two sulfate oxygen atoms occupying the axial sites. The covalent linkage between metals via the sulfate group, forming infinite 1D zigzag chains, ensures the entanglement of the structure. These chains, in turn, are further assembled into a 2D network through N-H...O hydrogen bonding. Thermal analyses underline the high thermal stability of our com…
1,2-Dihydropyrazole[1,2-a]benzo[1,2,4]triazine-3-one: deaza analogue tricyclic scaffold with valuable antiproliferative activity
2012
Dipeptides of S-Substituted Dehydrocysteine as Artzyme Building Blocks: Synthesis, Complexing Abilities and Antiproliferative Properties †
2021
Background: Dehydropeptides are analogs of peptides containing at least one conjugate double bond between α,β-carbon atoms. Its presence provides unique structural properties and reaction centre for chemical modification. In this study, the series of new class of dipeptides containing S-substituted dehydrocysteine with variety of heterocyclic moieties was prepared. The compounds were designed as the building blocks for the construction of artificial metalloenzymes (artzymes). Therefore, the complexing properties of representative compounds were also evaluated. Furthermore, the acknowledged biological activity of natural dehydropeptides was the reason to extend the study for antiproliferativ…
Synthesis and antiproliferative activity of the ring system [1,2]oxazolo[4,5-g]indole.
2012
Brand new ring: A series of 27 derivatives of the new ring system [1,2]oxazolo[4,5-g]indole were conveniently prepared and tested at the NCI for antiproliferative studies. Several of them showed good inhibitory activity toward all tested cell lines, reaching GI50 values generally at the micromolar and sub-micromolar levels and in some cases at nanomolar concentrations. The mean GI50 values, calculated on the full panel, were in the range 0.25-7.08 μM.
3-(6-Phenylimidazo [2,1-b][1,3,4]thiadiazol-2-yl)-1H-Indole Derivatives as New Anticancer Agents in the Treatment of Pancreatic Ductal Adenocarcinoma
2020
A new series of imidazo[2,1-b][1,3,4]thiadiazole derivatives was efficiently synthesized and screened for their in vitro antiproliferative activity on a panel of pancreatic ductal adenocarcinoma (PDAC) cells, including SUIT-2, Capan-1 and Panc-1. Compounds 9c and 9l, showed relevant in vitro antiproliferative activity on all three pre-clinical models with half maximal inhibitory concentration (IC50) ranging from 5.11 to 10.8 µ
1-methil-3H-pyrazolo[1-2-a]benzo[1-2-3-4]tetrazin-3-ones, design synthesis and biological activity of new antitumoral agents
2005
1-Methylpyrazolo[1,2-a]benzo[1,2,3,4]tetrazin-3-ones 4, synthesized in good to excellent yields, were designed as novel alkylating agents because of their peculiar chemical behavior. All derivatives showed antiproliferative activity against more than 50 types of tumor cell lines with GI50 reaching sub-micromolar values. SAR studies revealed that the presence of a chlorine atom is well-tolerated in both positions 8 and 9, whereas in the case of the methyl group, switching from the 8 to the 9 position gives rise to the most active compound of the series, 4g, either for the number of cell lines inhibited and for selectivity against leukaemia and renal cancer subpanels. COMPARE and 3D-MIND comp…
Synthesis and biological evaluation of new imidazo[2,1-b][1,3,4]thiadiazole derivatives: as anticancer and antibiofilm agents, and preclinical invest…
2020
Synthesis and Antitumor Activity of New Thiazole Nortopsentin Analogs
2016
New thiazole nortopsentin analogs in which one of the two indole units was replaced by a naphthyl and/or 7-azaindolyl portion, were conveniently synthesized. Among these, three derivatives showed good antiproliferative activity, in particular against MCF7 cell line, with GI50 values in the micromolar range. Their cytotoxic effect on MCF7 cells was further investigated in order to elucidate their mode of action. Results showed that the three compounds act as pro-apoptotic agents inducing a clear shift of viable cells towards early apoptosis, while not exerting necrotic effects. They also caused cell cycle perturbation with significant decrease in the percentage of cells in the G0/G1 and S ph…
3-(6-Phenylimidazo [2,1-
2019
A new series of imidazo[2,1-b][1,3,4]thiadiazole derivatives was efficiently synthesized and screened for their in vitro antiproliferative activity on a panel of pancreatic ductal adenocarcinoma (PDAC) cells, including SUIT-2, Capan-1 and Panc-1. Compounds 9c and 9l, showed relevant in vitro antiproliferative activity on all three pre-clinical models with half maximal inhibitory concentration (IC50) ranging from 5.11 to 10.8 µM, while the compounds 9e and 9n were active in at least one cell line. In addition, compound 9c significantly inhibited the migration rate of SUIT-2 and Capan-1 cells in the scratch wound-healing assay. In conclusion, our results will support further studies to increa…