O’Boyle, Niamh M. published the artcileSynthesis and Evaluation of Azetidinone Analogues of Combretastatin A-4 as Tubulin Targeting Agents, Synthetic Route of 1860-58-8, the publication is Journal of Medicinal Chemistry (2010), 53(24), 8569-8584, database is CAplus and MEDLINE.
The synthesis and antiproliferative activity of a new series of rigid analogs of combretastatin A-4 are described which contain the 1,4-diaryl-2-azetidinone (¦Â-lactam) ring system in place of the usual ethylene bridge present in the natural combretastatin stilbene products. These novel compounds are also substituted at position 3 of the ¦Â-lactam ring with an aryl ring. A number of analogs showed potent nanomolar activity in human MCF-7 and MDA-MB-231 breast cancer cell lines, displayed in vitro inhibition of tubulin polymerization, and did not cause significant cytotoxicity in normal murine breast epithelial cells. 4-(4-Methoxyphenyl)-substituted compound, 4-(3-hydroxy-4-methoxyphenyl)-substituted compounds, and the 3-(4-aminophenyl)-substituted compounds displayed the most potent antiproliferative activity of the series. ¦Â-Lactam I in particular showed subnanomolar activity in MCF-7 breast cancer cells (IC50 = 0.8 nM) together with significant in vitro inhibition of tubulin polymerization and has been selected for further biochem. assessment. These novel ¦Â-lactam compounds are identified as potentially useful scaffolds for the further development of antitumor agents that target tubulin.
Journal of Medicinal Chemistry published new progress about 1860-58-8. 1860-58-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ether, name is 2-(3-(Benzyloxy)phenyl)acetic acid, and the molecular formula is C15H14O3, Synthetic Route of 1860-58-8.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia