Discovery Of A Novel Series Of Imidazopyrazine Derivatives As Potent

Computer Aided Drug Discovery Novel 3 9 Disubstituted Eudistomin U We report here the identification of a novel series of shp2 allosteric inhibitors having an imidazopyrazine 6,5 fused heterocyclic system as the central scaffold that displays good potency in enzymatic and cellular assays. sar studies led to the identification of compound 8, a highly potent shp2 allosteric inhibitor. x ray studies showed novel. Discovery of a novel series of imidazopyrazine derivatives as potent shp2 allosteric inhibitors. sign in | create an account. orcid.org. europe pmc. menu.

Discovery Of A Novel Series Of Imidazopyrazine Derivatives As Potent Discovery of a novel series of imidazopyrazine derivatives as potent shp2 allosteric inhibitors. esther torrente *, valentina fodale, alina ciammaichella, federica ferrigno, jesus m. ontoria, simona ponzi, ilaria rossetti, alessio sferrazza, jérôme amaudrut, antonino missineo, simone esposito, simone palombo, martina nibbio, mauro cerretani. Through structural optimization and ring fusion strategy, we designed a series of novel imidazo[1,2 a]pyrazine derivatives as potential tubulin inhibitors. these compounds displayed potent anti proliferative activities (micromolar to nanomolar) against a panel of cancer cell lines (including hepg 2, hct 116, a549 and mda mb 231 cells). The success of targeted covalent inhibitors (tcis) for treating cancers has spurred the search for novel scaffolds to install covalent warheads. in our endeavour, using a scaffold hopping strategy, we managed to utilize imidazo[1,2 a]pyridine as the core backbone and explored its potential for the developmen. We report the discovery of a series of imidazo[1,2 a]pyrazine derivatives as novel inhibitors of phosphodiesterase 10a (pde10a). in a high throughput screening campaign we identified the imidazopyrazine derivative 1, a pde10a inhibitor with limited selectivity versus the other phosphodiesterases (pdes). subsequent investigation of 1 and replacement of the trimethoxyphenyl group by a.

Irbmтащs Drug юааdiscoveryюаб Research Is Featured On The Cover Of This Issueтащs The success of targeted covalent inhibitors (tcis) for treating cancers has spurred the search for novel scaffolds to install covalent warheads. in our endeavour, using a scaffold hopping strategy, we managed to utilize imidazo[1,2 a]pyridine as the core backbone and explored its potential for the developmen. We report the discovery of a series of imidazo[1,2 a]pyrazine derivatives as novel inhibitors of phosphodiesterase 10a (pde10a). in a high throughput screening campaign we identified the imidazopyrazine derivative 1, a pde10a inhibitor with limited selectivity versus the other phosphodiesterases (pdes). subsequent investigation of 1 and replacement of the trimethoxyphenyl group by a. Cdk4 6 has been identified as an attractive therapeutic target for treatment of cancer. for unmet clinical needs, a novel class of imidazo [1',2':1,6]pyrido [2,3 d]pyrimidin derivatives, which had distinctive triheteroaryl structure, had been discovered as cdk4 6 inhibitors. the compounds 10b and 10 …. We report the discovery of a series of imidazo[1,2 a]pyrazine derivatives as novel inhibitors of phosphodiesterase 10a (pde10a). in a high throughput screening campaign we identified the imidazopyrazine derivative 1, a pde10a inhibitor with limited selectivity versus the other phosphodiesterases (pdes).

Discovery Of Novel And Potent Tacrine Derivatives As Cdk2 Inhibitors Cdk4 6 has been identified as an attractive therapeutic target for treatment of cancer. for unmet clinical needs, a novel class of imidazo [1',2':1,6]pyrido [2,3 d]pyrimidin derivatives, which had distinctive triheteroaryl structure, had been discovered as cdk4 6 inhibitors. the compounds 10b and 10 …. We report the discovery of a series of imidazo[1,2 a]pyrazine derivatives as novel inhibitors of phosphodiesterase 10a (pde10a). in a high throughput screening campaign we identified the imidazopyrazine derivative 1, a pde10a inhibitor with limited selectivity versus the other phosphodiesterases (pdes).