1,721,049 research outputs found
Microwave-Assisted One-Pot Synthesis of Substituted Tetrahydrocarbazole and 8,9,10,11-Tetrahydro-7H-pyrido[a]carbazoles
No full textOne-pot synthesis of one-substituted tetrahydrocarbazole and 4-substituted 8,9,10,11-tetrahydro-7H-pyrido[a]carbazoles
from substituted quinolinylhydrazines and cyclohexanone in acetic acid was performed by microwave irradiation in a controlled
temperature with simultaneous cooling system in closed vessel. The optimization procedures of process variables, power, temperature,
and irradiation time are reported in detail, and the results from microwave processes are compared with conventional ones
Synthesis of some Mannich N-bases of triazoloquinolines as pharmacologically active compounds
No full textBologna (Italy
An overview on 2-arylquinolin-4(1h)-ones and related structures as tubulin polymerisation inhibitors
No full textAgents that interfere with tubulin function have a broad anti-tumour spectrum and they represent one of the most significant classes of anti-cancer agents. In the past few years, several small synthetic molecules that have an azaflavone nucleus as a core structure have been identified as tubulin inhibitors. Among these, several arylquinolinones, arylnaphthyridinones, arylquinazolinones and arylpyrroloquinolinones have shown to exert their anticancer activity through inhibition of tubulin polymerisation via the colchicine binding site. They arrest the cell growth at G2/M phase providing cell death via both mitotic and apoptotic pathway. Recently, some of them proved to be multi-inhibitor simultaneously targeting both PI3K-Akt-mTOR pathway and the microtubule cytoskeleton. Furthermore, some were demonstrated to possess effective anti-angiogenic properties similar to that of natural compounds combretastatine-A4 and vincristine. This article reviews the synthesis, biological activities and SARs of the main classes of azaflavones. Brief mention of the subtype 2styrylquinazolinones has also been made
Derivati fenilpirrolochinolinonici e loro uso come agenti antimitotici
No full textLa presente invenzione descrive il processo di sintesi e l’attività biologica antiproliferativa “in vitro” ed “in vivo” di nuovi agenti antitumorali a struttura 7-fenil-pirrolo[3,2-f]chinolinonica specificatamente sostituiti all’azoto pirrolico, in grado di interferire con la divisione cellulare, o mitosi, di cellule altamente proliferative tramite inibizione della polimerizzazione della tubulina. Tali agenti antimitotici presentano i seguenti vantaggi:
Facilità di sintesi, purificazione, d’uso e conservazione
Ridotto costo della sintesi, purificazione, uso e conservazione
Elevata citotossicità
Ridotti effetti collaterali indesiderati
3-substituted 7-phenyl-pyrroloquinolinones show potent cytotoxic activity in human cancer cell lines.
No full textA novel series of 3-alkyl-substituted 7-phenyl-3H-pyrrolo[3,2-f]quinolin-9-ones (7-PPyQs) was synthesized with the aim to optimize the cytotoxic activity of recently identified PPyQs, promising inhibitors of tubulin polymerization. All compounds inhibited the growth of 11 human tumor cell lines at submicromolar concentrations as well as two human resistant cancer sublines, A549-T12 and A549-T24. FACS analysis indicated that all compounds caused significant arrest of the A549 cell cycle in G2/M phase at 0.1 and 1 muM and a good correlation between the cytotoxicity IC50 and their ability to block the cell cycle was observed
Synthesis of some Mannich bases of 3H-pyrrolo[3,2-f]quinolibne
No full textGiardini Naxos-Taormina (Italy
Synthesis and Evaluation of Platelet Aggregation Inhibitory Activity of Some 3-Phenyl-pyrroloquinazolinones
No full textA series of 3-phenyl-2H-pyrrolo[3,2-f]quinazolin-1-one derivatives (3-PPyQZ) was synthesized starting from 5-amino-indoles, via condensation with N-ethoxycarbonylthiobezamides followed by thermal cyclisation. On the basis of their structural analogy with reported anti-thrombin pyrroloquinazolines, the derivatives were first tested for their capacity to inhibit platelet aggregation. Some of them had in vitro inhibitory effects on collagen and thrombin-induced aggregation in the micromolar range, and much higher inhibition than that shown by new phenyl-pyrroloquinolinones. Experiments to determine the mechanism of action of the most potent inhibitor (compound 18) indicated that it acts in at least two sites: one preceding the agonist-induced increase of cytosolic [Ca2+], and one following this step of the platelet activation cascade. The compound also inhibited thrombin-evoked protein-Tyr-phosphorylation. Although it is premature to draw definitive conclusions, the present results indicate that 3-PPyQZ structure, with the quite potent inhibitor of platelet aggregation compound 18, might constitute a starting point for the synthesis of potential anti-thrombosis agents
Structure-Activity Relationships of Phenylpyrroloquinolinones as Inhibitors of Tubulin Polymerization
No full text- …
