He, Fengming published the artcileDesign, synthesis, and biological evaluation of (E)-N’-substituted-4-((4-pyridylpyrimidin-2-yl)amino)benzohydrazide derivatives as novel potential CDK9 inhibitors, Formula: C9H10O3, the main research area is pyridylpyrimidinyl benzohydrazide preparation antitumor HIV inhibitor mol docking.
In a continuing effort to develop new CDK9 inhibitors endowed with good anticancer activity, a series of new benzene carbohydrazide derivatives I (R = pyridin-2-yl, pyridin-3-yl, pyridin-4-yl; R 1 = n-Pr, 4-methylphenyl, thiophen-2-yl, etc.) bearing a (pyridyl pyrimidin-2-yl)amino moiety in position-4 of the Ph ring was designed and synthesized. This work reports the preparation of benzene carbohydrazide derivatives I, their inhibition effect on HIV-1 transcription, and the preliminary structure-activity relationships. Compound I (R = pyridin-2-yl, R 1 = 4-methoxyphenyl (II)) was found to be the most potent CDK9 inhibitor and exhibited excellent anti-proliferative activities against cancer cells (A375, A549, HepG2, and MCF-7) but was less toxic to normal cells (MCF-10A and HaCaT). Further bioassays indicated that compound II could induce the apoptosis of cancer cells, which contributes to its antitumor effects. Finally, the mol. docking studies are performed to predict the binding mode of 9h at the ATP binding site of CDK9 and identify the essential amino acids responsible for the interactions.
Arabian Journal of Chemistry published new progress about Aldehydes 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, Formula: C9H10O3.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem