Lichitsky, Boris V. published the artcileBenzimidazolyl-pyrazolo[3,4-b]pyridinones – selective inhibitors of MOLT-4 leukemia cell growth and sea urchin embryo spiculogenesis: Target quest., Safety of 2,3-Dimethoxybenzaldehyde, the main research area is benzimidazolylpyrazolopyridinone preparation SAR human; MOLT4 leukemia cell growth spiculogenesis inhibitor; MOLT-4; benzimidazolyl-pyrazolo[3,4-b]pyridinone; cytotoxicity; sea urchin embryo; spiculogenesis.
1,3-Substituted pyrazolo[3,4-b]pyridinones were synthesized by a three-component condensation of Meldrum’s acid with aryl aldehydes and 1,3-substituted 5-aminopyrazoles. Their biol. activity was evaluated using the in vivo phenotypic sea urchin embryo assay and the in vitro cytotoxicity screen against human cancer cell lines. In the sea urchin embryo model, 1-benzimidazolyl-pyrazolo[3,4-b]pyridinones caused inhibition of hatching and spiculogenesis at submicromolar concentrations These compounds also selectively and potently inhibited growth of the MOLT-4 leukemia cell line. Subsequent structure-activity relationship studies determined the benzimidazolyl fragment as an essential pharmacophore for both effects. A preliminary QSAR target identification search did not result in tangible leads. Attempts to prepare a relevant photoaffinity probe that retained potency in both assays were not successful. 1-Benzimidazolyl-pyrazolo[3,4-b]pyridinones were further characterized for their activity in a wild type vs Notch-mutant leukemia cell lines, and in in vitro panels of kinases and matrix metalloproteinases. Using a series of diverse modulators of spiculogenesis as standards, multiple signaling networks including Notch, Wnt/-catenin, receptor tyrosine kinases (VEGF/VEGFR, FGF/FGFR), PI3K, and Raf-MEK-ERK were excluded as possible targets of 1-benzimidazolyl-pyrazolo[3,4-b]pyridinones. On the other hand, matrix metalloproteinase-9/hatching enzyme was identified as one potential target.
ACS Combinatorial Science published new progress about Benzaldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Safety of 2,3-Dimethoxybenzaldehyde.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem