Medicinal Chemistry

In the present review developed a new method for synthesis coumarin substituted chromone, as they are an important building block in organic chemistry. Also, they are valuable synthetic intermediates in the preparation of new biological relevant heterocyclic system have been synthesized by using effective and efficient synthetic pathway. The synthesized compound has been characterized by FT-IR, 1H-NMR, UV and Mass spectrometry for their structural elucidation. Further, we have studied their fluorescence properties.

Graphical Abstract

A series of N-substituted benzamide derivatives designed based on Entinostat (MS-275) were synthesized, and characterized by IR, MS, 1H NMR and 13C NMR. Their anti-proliferative activity in vitro against four cell lines including MCF-7, MDA-MB-231, K562 and A549 were also evaluated by the MTT assay, the results showed that several compounds displayed similar inhibitory activity compared with MS-275. Finally, binding affinity of the synthesized compounds towards targets (histone deacetylases, HDACs) was studied using molecular docking simulations, compounds 13h and 13k were observed hydrogen bond, Vander Waals bond and hydrophobic interactions with HDAC2 and HDAC8.