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Design, Synthesis and Cytotoxic Activity Evaluation of Newly Synthesized Amides-Based TMP Moiety as Potential Anticancer Agents over HepG2 Cells. | LitMetric

AI Article Synopsis

Article Abstract

A novel series of amides based TMP moiety was designed, synthesized and evaluated for their antiproliferative as well as enzyme inhibition activity. Compounds and showed remarkable cytotoxic activity against HepG2 cells with IC values 0.65 and 0.92 μM, respectively compared with SAHA and CA-4 as reference compounds. In addition, compound demonstrated good HDAC-tubulin dual inhibition activity as it showed better HDAC activity as well as anti-tubulin activity. Moreover, compound exhibited G2/M phase arrest and pre-G1 apoptosis as demonstrated by cell cycle analysis and Annexin V assays. Further apoptosis studies demonstrated that compound boosted the level of aspase 3/7. aspase 3/7 activation and apoptosis induction were evidenced by decrease in mitochondrial permeability suggesting that activation of aspase 3/7 may occur via mitochondrial apoptotic pathway.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9227250PMC
http://dx.doi.org/10.3390/molecules27123960DOI Listing

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