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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 ...
[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 ...
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 ...
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 ...
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 ...
[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.
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 ...
Phytochemical screening and repellence potencies of bioactive molecules of plant extracts derived from Ocimum suave, Ocimum americanum and Eucalyptus citriodora against Anopheles gambiae
(Malaria Journal, 2025)
Background Malaria poses a global threat to human health. It’s a vector-borne disease of public health concern and afects the socio-economic status of people in developing countries. Malaria management faces many challenges ...