74229-12-2Relevant academic research and scientific papers
Expanding the chemical space: Discovery of new anticancer 3-arylbenzofuran derivatives
Bae, Gi H.,Cha, Hyeon-Min,Kim, Ikyon,Kim, Jinhwang,Kim, Seong H.,Park, Mikyung,Singh, Dileep K.
, p. 3279 - 3293 (2020)
A new chemical space was generated via C2-functionalization of 3-arylbenzofurans. Mannich reaction of 3-arylbenzofurans with secondary amines and formaldehyde allowed for installation of aminomethyl unit at C2 position of benzofurans. A formyl group at C2 site introduced as a result of Vilsmeier-Haack formylation of 3-arylbenzofurans was employed as a reacting partner for three-component Kabachnik-Fields reaction with various amines and triethyl phosphite to give a wide variety of aminomethylphosphonates. Furthermore, several benzo[d]oxazoles and pyrrolo[1,2-a]quinoxalines were prepared by using the formyl group. Biological screening of the synthesized compounds revealed that the benzofuran bearing a pyrrolo[1,2-a]quinoxaline moiety (5b) most potently inhibited the viability of human blood cancer cells, but not solid tumor cells. Caspase activity assay, analysis of Annexin V-positive cells, and Western blot analysis indicated that 5b-induced death of human lymphoma U937 cells could result from its potential to induce the caspase-dependent apoptotic death of blood cancer cells with inhibition of ERK activation.
novel benzofuran compound and anticancer composition comprising the same
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Paragraph 0209-0215; 0216-0218, (2021/05/04)
The present invention provides a novel benzofuran compound, a solvate thereof, a hydrate thereof, a predrug thereof, an isomer thereof or a pharmaceutically acceptable salt thereof, and an anticancer composition comprising the same, wherein the novel benzofuran compound of the present invention is very useful for preventing and treating cancer by introducing a specific substituent at a specific position in the 3-aryl benzofuran backbone.
