Hassan, Aisha Y. published the artcilePotential antiviral and anticancer effect of imidazoles and bridgehead imidazoles generated by HPV-Induced cervical carcinomas via reactivating the P53/pRb pathway and inhibition of CA IX, Application of 2-Chloroacetamide, the publication is Journal of Molecular Structure (2021), 129865, database is CAplus.
Human papillomaviruses E6 and E7 oncoproteins are crucial to viral-induced cervical cancers and targeting E6/E7 leads to safer and better treatment for cervical cancer. Hence, a simple and green solvent-free protocol was applied for the synthesis of novel imidazoles e.g., I, and bridgehead imidazoles (purine analogs), e.g., II, via versatile straightforward synthetic routes. All the synthesized compounds have been characterized by IR, 1H NMR, 13C NMR, mass spectroscopy, and elemental analyses and then have been examined for their in vitro antiviral activity against HPV, genotype 18. Two compounds, I and II, were the most promising HR-HPV inhibitors with a percentage of 95.00 and 96.84%, resp. Both compounds demonstrated a substantial down-regulation of HPV oncoproteins E6 and E7 with up-regulation of tumor suppressor proteins, p53, and pRb, resp. using western blot technique. Furthermore, the cytotoxicity of compounds I and II against the cervical cancer Hela cell line was further examined Compound I exhibited strong anticancer activity with IC50 0.08μM, which is equivalent to 5-FU (IC50 0.09μM). The cell cycle anal. was performed for investigating the potential mechanism of compound I, resulting in a significant accumulation of the cell population in both pre-G1 and G0-G1 phases and arrest the cell cycle at G1 phase. Addnl., compound I induced apoptosis, triggering cell death via increasing the early and late apoptotic rates by approx. 16 and 188 folds compared with the control. The most cytotoxic agent, I, revealed a remarkable inhibition of the targeted carbonic anhydrase IX enzyme with an IC50 value of 0.12μM comparable to the standard drug. In addition, the ADME profiles of the most highly successful derivatives have been studied in order to determine their ability to be produced as good drug candidates.
Journal of Molecular Structure published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Application of 2-Chloroacetamide.
Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics