Sun, Wenxue published the artcileDesign, semi-synthesis and bioactivity evaluation of novel podophyllotoxin derivatives as potent anti-tumor agents, COA of Formula: C10H10O3, the publication is Bioorganic Chemistry (2022), 105906, database is CAplus and MEDLINE.
In this study, a series of potential candidate mols. with excellent antitumor activity targeting tubulin and PTEN/PI3K/Akt signaling pathway was synthesized by modifying the mol. structure of podophyllotoxin (PPT) at the C-4 position via a structure-guided drug design approach. MTT assay results indicated that compound 12c had stronger anti-proliferative activities against HGC-27, MCF-7 and H460 cell lines than etoposide (VP-16), especially for HGC-27 (12c: IC50 = 0.89 ¡À 0.023 ¦ÌM; PPT: IC50 = 6.54 ¡À 0.69 ¦ÌM, VP-16: IC50 = 2.66 ¡À 0.28 ¦ÌM) with lower affect in healthy human cells (293 T and GES-1). Further pharmacol. anal. exhibited that 12c could bind the tubulin at the colchicine site and disrupt the dynamic equilibrium of microtubules. Moreover, 12c also suppressed the expressions/activities of matrix metalloprotease (MMP)-2, vimentin and up-regulation E-cadherin suggesting that 12c could block the epithelial-mesenchymal transition (EMT). The increased cell survival and invasion/migration were associated with the inactivation of PTEN/PI3K/Akt, 12c could regulate this pathway and cascade influence on the mitochondrial pathway, eventually, leading to the cell apoptosis. Thus, 12c may have the potential to become a candidate mol. in gastric cancer clin. treatment.
Bioorganic Chemistry published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C13H13BO2S, COA of Formula: C10H10O3.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia