Phthalazinone Pyrazoles as Potent, Selective, and Orally Bioavailable Inhibitors of Aurora-A Kinase was written by Prime, Michael E.;Courtney, Stephen M.;Brookfield, Frederick A.;Marston, Richard W.;Walker, Victoria;Warne, Justin;Boyd, Andrew E.;Kairies, Norman A.;von der Saal, Wolfgang;Limberg, Anja;Georges, Guy;Engh, Richard A.;Goller, Bernhard;Rueger, Petra;Rueth, Matthias. And the article was included in Journal of Medicinal Chemistry in 2011.Electric Literature of C5H6BrNS The following contents are mentioned in the article:
The inhibition of Aurora kinases in order to arrest mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells has generated significant discussion within the literature. We report a novel class of Aurora kinase inhibitors based upon a phthalazinone pyrazole scaffold. The development of the phthalazinone template resulted in a potent Aurora-A selective series of compounds (typically >1000-fold selectivity over Aurora-B) that display good pharmacol. profiles with significantly improved oral bioavailability compared to the well studied Aurora inhibitor VX-680. This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Electric Literature of C5H6BrNS).
4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Electric Literature of C5H6BrNS
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica