Ashida, Yoshiki; Yanagita, Ryo C.; Kawanami, Yasuhiro; Okamura, Mutsumi; Dan, Shingo; Irie, Kazuhiro published the artcile< Synthesis, conformation and biological activities of a des-a-ring analog of 18-deoxy-aplog-1, a simplified analog of debromoaplysiatoxin>, Related Products of 128-09-6, the main research area is protein kinase 18 deoxy aplog1 analog neoplasm antiproliferative activity.
10-Me-Aplog-1 as a simplified analog of tumor-promoting debromoaplysiatoxin and a potent activator of protein kinase C (PKC) is a promising chemotherapeutic agent. In this study, we synthesized a des-A-ring analog of 18-deoxy-aplog-1 as a synthetically-accessible analog. Compound 4 retained the conformation of the PKC-recognition part of aplogs. Moderate affinity for conventional PKC isoenzymes (α, β, γ) and anti-proliferative activity against NCI-H460 (lung) and MKN45 (stomach) human cancer cell lines were observed The results suggest that 4 could serve as a lead compound for the development of conventional PKC isoenzyme-selective chemotherapeutic agents.
Heterocycles published new progress about Antitumor agents. 128-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C4H4ClNO2, Related Products of 128-09-6.
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