Meegan, Mary J. published the artcilePiperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents, Safety of (E)-3-(2,4-Dimethoxyphenyl)acrylic acid, the publication is European Journal of Medicinal Chemistry (2017), 453-463, database is CAplus and MEDLINE.
Piperlongumine (piplartine, 1) is a small mol. alkaloid that is receiving intense interest due to its antiproliferative and anticancer activities. We investigated the effects of 1 on tubulin and microtubules. Using both an isolated tubulin assay, and a combination of sedimentation and western blotting, we demonstrated that 1 is a tubulin-destabilizing agent. This result was confirmed by immunofluorescence and confocal microscopy, which showed that microtubules in MCF-7 breast cancer cells were depolymerized when treated with 1. We synthesized a number of analogs of 1 to explore structure-activity relationships. Compound 13 had the best cytotoxic profile of this series, showing potent effects in human breast carcinoma MCF-7 cells while being relatively non-toxic to non-tumorigenic MCF-10a cells. These compounds will be further developed as potential clin. candidates for the treatment of breast cancer.
European Journal of Medicinal Chemistry published new progress about 16909-09-4. 16909-09-4 belongs to catalysis-chemistry, auxiliary class Alkenyl,Carboxylic acid,Benzene,Ether, name is (E)-3-(2,4-Dimethoxyphenyl)acrylic acid, and the molecular formula is C11H12O4, Safety of (E)-3-(2,4-Dimethoxyphenyl)acrylic acid.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia