21288-34-6Relevant articles and documents
SUBSTITUTED PYRIDINES AS INHIBITORS OF DNMT1
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Page/Page column 839, (2018/01/20)
The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors
Wityak, John,Hobbs, Frank W.,Gardner, Daniel S.,Santella III, Joseph B.,Petraitis, Joseph J.,Sun, Jung-Hui,Favata, Margaret F.,Daulerio, Andrea J.,Horiuchi, Kurumi Y.,Copeland, Robert A.,Scherle, Peggy A.,Jaffe, Bruce D.,Trzaskos, James M.,Magolda, Ronald L.,Trainor, George L.,Duncia, John V.
, p. 1483 - 1486 (2007/10/03)
Employing phenylmalonitrile dianion chemistry, a large number of analogues of MEK inhibitor lead SH053 (IC50=140 nM) were rapidly synthesized leading to single digit nM inhibitors, displaying submicromolar AP-1 transcription inhibition in COS-7 cells. Compound 41, exhibiting a MEK IC 50=12 nM showed ip activity in a TPA-induced ear edema model with an ED50=5 mg/kg.
Efficient photodecarboxylation of aroyl-substituted phenylacetic acids in aqueous solution: A general photochemical reaction
Xu,Wan
, p. 2147 - 2148 (2007/10/03)
Photolysis (254-350 nm) of a variety of aroyl-substituted phenylacetic acids and p-acetylphenylacetic acid in aqueous solution at pH > pK(a) resulted in efficient photodecarboxylation (Φ = 0.2-0.7), to give in most cases a single product arising via the corresponding arylmethyl carbanion, indicating that photodecarboxylation is an efficient and general reaction for these types of compounds.