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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 ...
Stereoselective synthesis of fused tetrahydroquinazolines through one-pot double [3 + 2] dipolar cycloadditions followed by [5 + 1] annulation
(2016-10)
The one-pot [3 + 2] cycloaddition of an azomethine ylide with a maleimide followed by another [3 + 2] cycloaddition of an azide with the second maleimide gives a 1,5-diamino intermediate which is used for a sequential ...
[3 + 2] Cycloaddition and Cascade Radical Reactions for the Synthesis of Trifluoromethylated Tetrahydrobenzodiazepin-3-ones
(2019-04-01)
A reaction sequence involving three-component [3 + 2] cycloaddition of azomethine ylides followed by CuI catalyzed cascade trifluoromethyl radical addition and cyclization is developed for diastereoselective synthesis of ...
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 ...
[3+2] Cycloaddition-based one-pot synthesis of 3,9-diazabicyclo[4.2.1]nonane-containing scaffold
(2017-01)
Three-component [3+2] cycloaddition followed by reduction and lactamization has been developed as a one-pot methodology for diastereoselective synthesis of 3,9-diazabicyclo[4.2.1]nonane-containing scaffold.