Li, Qing’s team published research in Bioorganic & Medicinal Chemistry Letters in 2020-05-15 | CAS: 104-01-8

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Related Products of isoquinoline.

Li, Qing published the artcileSynthesis of (1,3,4-thiadiazol-2-yl)-acrylamide derivatives as potential antitumor agents against acute leukemia cells, Related Products of isoquinoline, the main research area is thiadiazole acrylamide preparation antitumor leukemia caspase dependent apoptosis; (1,3,4-thiadiazol-2-yl)-acrylamide; Acute leukemia; Antitumor agents; Cell apoptosis; Cytotoxicity.

A lead compound with the (1,3,4-thiadiazol-2-yl)-acrylamide scaffold was discovered to have significant cytotoxicity on several tumor cell lines in an inhouse cell-based screening. A total of 60 derivative compounds were then synthesized and tested in a CCK-8 cell viability assay. Some of them exhibited improved cytotoxic activities. The most potent compounds had IC50 values of 1-5μM on two acute leukemia tumor cell lines, i.e. RS4;11 and HL-60. Flow cytometry anal. of several active compounds and detection of caspase activation indicated that they induced caspase-dependent apoptosis. It was also encouraging to observe that these compounds did not have obvious cytotoxicity on normal cells, i.e. IC50 > 50μM on HEK-293T cells. Although the mol. targets of this class of compound are yet to be revealed, our current results suggest that this class of compound represents a new possibility for developing drug candidates against acute leukemia.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Related Products of isoquinoline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem