1402344-73-3Relevant academic research and scientific papers
Ethylenediamine diacetate (EDDA) mediated synthesis of aurones under ultrasound: Their evaluation as inhibitors of SIRT1
Manjulatha, Khanapur,Srinivas,Mulakayala, Naveen,Rambabu,Prabhakar,Arunasree, Kalle M.,Alvala, Mallika,Basaveswara Rao,Pal, Manojit
, p. 6160 - 6165 (2012/10/30)
An improved synthesis of functionalized aurones has been accomplished via the reaction of benzofuran-3(2H)-one with a range of benzaldehydes in the presence of a mild base EDDA under ultrasound. A number of aurones were synthesized (within 5-30 min) and the molecular structure of a representative compound determined by single crystal X-ray diffraction study confirmed Z-geometry of the C-C double bond present within the molecule. Some of the compounds synthesized have shown SIRT1 inhibiting as well as anti proliferative properties against two cancer cell lines in vitro. Compound 3a [(Z)-2-(5-bromo-2-hydroxybenzylidene) benzofuran-3(2H)-one] was identified as a potent inhibitor of SIRT1 (IC50 = 1 μM) which showed a dose dependent increase in the acetylation of p53 resulting in induction of apoptosis.
