Kostrzewa, Tomasz; Wolosewicz, Karol; Jamrozik, Marek; Drzezdzon, Joanna; Sieminska, Julia; Jacewicz, Dagmara; Gorska-Ponikowska, Magdalena; Kolaczkowski, Marcin; Lazny, Ryszard; Kuban-Jankowska, Alicja published their research in International Journal of Molecular Sciences in 2021. The article was titled 《Curcumin and Its New Derivatives: Correlation between Cytotoxicity against Breast Cancer Cell Lines, Degradation of PTP1B Phosphatase and ROS Generation》.Electric Literature of C6H11NO The article contains the following contents:
Breast cancer is the most common cancer of women-it affects more than 2 million women worldwide. PTP1B phosphatase can be one of the possible targets for new drugs in breast cancer therapy. In this paper, we present new curcumin derivatives featuring a 4-piperidone ring as PTP1B inhibitors and ROS inducers. We performed cytotoxicity anal. for twelve curcumin derivatives against breast cancer MCF-7 and MDA-MB-231 cell lines and the human keratinocyte HaCaT cell line. Furthermore, because curcumin is a known antioxidant, we assessed antioxidant effects in its derivatives For the most potent cytotoxic compounds, we determined intracellular ROS and PTP1B phosphatase levels. Moreover, for curcumin and its derivatives, we performed real-time microscopy to observe the photosensitizing effect. Finally, computational anal. was performed for the curcumin derivatives with an inhibitory effect against PTP1B phosphatase to assess the potential binding mode of new inhibitors within the allosteric site of the enzyme. We observed that two tested compounds are better anticancer agents than curcumin. Moreover, we suggest that blocking the -OH group in phenolic compounds causes an increase in the cytotoxicity effect, even at a low concentration Furthermore, due to this modification, a higher level of ROS is induced, which correlates with a lower level of PTP1B. The results came from multiple reactions, including the reaction of 1-Methyl-4-piperidone(cas: 1445-73-4Electric Literature of C6H11NO)
1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Electric Literature of C6H11NO
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem