14256-74-7Relevant articles and documents
DUAL ATM AND DNA-PK INHIBITORS FOR USE IN ANTI-TUMOR THERAPY
-
Page/Page column 376; 377, (2019/11/12)
Provided herein are compounds of the Formula (I), (II), and (III), as well as pharmaceutically acceptable salts thereof, wherein the substituents are those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of oncologic diseases.
TOLL-LIKE RECEPTOR-7 AGONIST
-
Paragraph 0100-0101, (2018/06/09)
Disclosed are a novel pyrrolopyrimidine ring compound as a TLR7 agonist or a pharmaceutically acceptable salt thereof, used for preventing or treating allergic rhinitis and asthma. In particular, disclosed is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
USE OF EMICORONS AS SELECTIVE INDUCERS OF DAMAGE TO THE TELOMERE DNA
-
Page/Page column 32; 33, (2014/05/07)
The hydrosoluble emicoron derivatives of the general formula (I) are particularly effective as inducers of selective telomere and non- telomere DNA damage in tumour and transformed cells. The damage is measured as the ability to cause a number of TIF foci in transformed cells that is equal to or higher than 4 at a 0.1 uM dose of the compound of the formula (I). Such emicoron derivatives can be used in a kit together with other known anti-tumour drugs, such as, for example, topoisomerase I inhibitors, for the combined, simultaneous, delayed or sequential administration. The emicoron compounds of the formula (I) are particularly useful in the therapy of tumours that do not express p53 protein or express an inactive p53 protein and of tumours that maintain telomeres by mechanisms different from telomere maintenance by telomerase, and in the removal of cancer stem cells. Also, the method for the preparation of emicoron compounds of the formula (I), which envisages the use of intermediates such as the Ν,Ν'-bis [2-(1-piperidino)-ethyl] - 1-(1-piperidinyl)-7- [3-(1-piperidino)- butynyl]-perylene-3,4;9,10-tetracarboxyl diimide, is described.
Diamine-based human histamine H3 receptor antagonists: (4-Aminobutyn-1-yl)benzylamines
Dvorak, Curt A.,Apodaca, Richard,Xiao, Wei,Jablonowski, Jill A.,Bonaventure, Pascal,Dugovic, Christine,Shelton, Jonathan,Lord, Brian,Miller, Kirsten,Dvorak, Lisa K.,Lovenberg, Timothy W.,Carruthers, Nicholas I.
experimental part, p. 4098 - 4106 (2009/12/06)
A series of (4-aminobutyn-1-yl)benzylamines were prepared and the SAR around three key areas: (1) the amine attached to the butynyl linker (R3R4N-); (2) the benzylamine moiety (R1R2N-); and (3) the point of attachment of the benzylamine group (R1R2N- in the ortho, meta, or para positions) was examined. One compound, 4-[3-(4-piperidin-1-yl-but-1-ynyl)-benzyl]-morpholine (9s) was chosen for further profiling and found to be a selective histamine H3 antagonist with desirable drug-like properties. Ex vivo receptor occupancy studies established that 9s does occupy H3 binding sites in the brain of rats after oral administration. Subcutaneous doses of 9s (10 mg/kg) given during the natural sleep phase demonstrated robust wake-promoting effects.
A two-step, formal [4 + 2] approach toward piperidin-4-ones via au catalysis
Cui, Li,Peng, Yu,Zhang, Liming
supporting information; experimental part, p. 8394 - 8395 (2009/10/23)
(Chemical Equation Presented) An efficient, formal [4 + 2] synthesis of synthetically valuable piperidin-4-ones from secondary amines in two steps has been achieved via a key gold catalysis without the purification of tertiary amine intermediates. This reaction is selective toward the less-substituted alkyl group and shows moderate to excellent diastereoselectivities. Its synthetic potential in alkaloid synthesis is demonstratedin a highly diastereoselective synthesis of (±)-cermizine C.
WATER-SOLUBLE CORONENE DERIVATIVES ACTIVE AS INHIBITORS OF HUMAN TELOMERASE BY INDUCTION OF G-QUADRUPLEX STRUCTURES AND THEIR USE AS ANTICANCER AGENTS
-
Page/Page column 25-26, (2008/12/08)
The coronene derivatives of general formula: (I); wherein R1, R2, R2', R3, R4 and R4', when present and different from H, represent hydrophilic chains, constitute a new family of compounds that can selectively induce the formation of G-quadruplex structures in the telomeric DNA, and can thus act as inhibitors of the telomerase enzyme, thereby inhibiting tumour proliferation. These compounds proved to have a strong anticancer activity in vitro, which was assessed with many human tumour cell lines. Preparations including the coronene derivatives of formula (I) as active ingredients are proposed as medicament for use in anticancer treatments.
Specific interactions with intra- and intermolecular G-quadruplex DNA structures by hydrosoluble coronene derivatives: A new class of telomerase inhibitors
Franceschin, Marco,Alvino, Antonello,Casagrande, Valentina,Mauriello, Clementina,Pascucci, Emanuela,Savino, Maria,Ortaggi, Giancarlo,Bianco, Armandodoriano
, p. 1848 - 1858 (2008/02/03)
In developing G-quadruplex interactive telomerase inhibitors two main features have to be taken into account: the hydrophobic interactions with the G-quartet plane and the electrostatic interactions with the negatively charged phosphates of the four grooves. In this paper, we report the synthesis of four hydrosoluble coronene derivatives, which are characterized by a large hydrophobic aromatic core and four orthogonal hydrophilic side chains. We have studied their ability to induce both inter- and intramolecular G-quadruplex structures and found a significant selectivity of all the coronene derivatives for the intramolecular G-quadruplex. The efficiency in inhibiting human telomerase has been evaluated in a cell-free system and the experimental results correlate with the relative affinities of these compounds for the G-quadruplex monomeric structure, as derived by molecular modelling simulations. Thus, the coronene derivatives can be considered as a new class of telomerase inhibitors, although further investigations are surely necessary to fully exploit their features.
Aminomethylation of organic halides promoted by zinc in protic medium
Estevam, Idália H. S.,Da Silva, Margarete F.,Bieber, Lothar W.
, p. 7601 - 7604 (2007/10/03)
Organic halides undergo smooth aminomethylation by secondary amines and aqueous formaldehyde promoted by metallic zinc under copper(I) catalysis. Good to excellent yields are obtained with primary, secondary, and tertiary iodides, allylic, propargylic, and benzylic bromides and with α-bromoesters. In most cases, DMSO is the best solvent, but dioxane is preferable for some more reactive halides. Additional experiments with radical quenchers and promoters and the use of 'radical clocks' indicate a stepwise reaction mechanism initiated by the attack of an alkyl radical to iminium ion.
New hydrosoluble perylene and coronene derivatives
Franceschin, Marco,Alvino, Antonello,Ortaggi, Giancarlo,Bianco, Armandodoriano
, p. 9015 - 9020 (2007/10/03)
Several lipophilic perylene and coronene derivatives, employed mainly as liquid crystalline dyes are known and their synthesis has been widely studied. We have applied an analogue strategy using hydrophilic substituents to obtain highly water soluble perylene diimides (4) and a new hydrosoluble coronene derivative (CORON, 6), whose molecular features appear particularly suitable for inducing G-quadruplex DNA structures and inhibiting human telomerase.
Phenylalkynes
-
, (2008/06/13)
Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
