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Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors
(2018)
The simultaneous inhibition of polo-like kinase 1 (PLK1) and BRD4 bromodomain by a single molecule
could lead to the development of an effective therapeutic strategy for a variety of diseases in which PLK1 and BRD4 are ...
Development of Dimethylisoxazole-Attached Imidazo[1,2‑a]pyridines as Potent and Selective CBP/P300 Inhibitors
(2021)
The use of epigenetic bromodomain inhibitors as anticancer therapeutics has transitioned from targeting bromodo main extraterminal domain (BET) proteins into targeting non-BET bromodomains. The two most relevant non-BET ...
One-pot and catalyst-free synthesis of pyrroloquinolinediones and quinolinedicarboxylates†
(2017)
A method for the catalyst-free synthesis of pyrroloquinolinediones and quinolinedicarboxylates is develo ped through a one-pot synthesis involving denitrogenation of azide, benzisoxazole formation, aza-Diels–
Alder ...
Sequential (3 + 2) cycloaddition and (5 + n) annulation for modular synthesis of dihydrobenzoxazines, tetrahydrobenzoxazepines and tetrahydrobenzoxazocines†
(2018-06)
A two-step method for the (3 + 2) cycloaddition of azomethine ylides followed by a double SN2 substi tution-based (5 + n) annulation is introduced for the modular synthesis of dihydrobenzoxazine, tetra hydrobenzoxazepine ...