On February 25, 2022, Ochi, Akihiro; Yoritate, Makoto; Miyamoto, Tomofumi; Usui, Kazuteru; Yusakul, Gorawit; Putalun, Waraporn; Tanaka, Hiroyuki; Hirai, Go; Morimoto, Satoshi; Sakamoto, Seiichi published an article.Application In Synthesis of tert-Butyl trichloroacetimidate The title of the article was Harringtonine Ester Derivatives with Enhanced Antiproliferative Activities against HL-60 and HeLa Cells. And the article contained the following:
Harringtonine (HT), produced from Cephalotaxus species, is known to exhibit potent antiproliferative activity against myeloid leukemia cells by inhibiting protein synthesis. A previous study using acute promyelocytic leukemia (HL-60) cells raised the possibility that the C-5′ Me group of HT plays an important role in regulating leukemia cell line antiproliferative activity. In order to investigate the effect of hydrocarbon chains at C-5′ on the resultant activity, the C-5′ Me group was replaced with various straight- and branched-chain hydrocarbons using the corresponding alcs., and their antiproliferative activity against HL-60 and HeLa cells was investigated. As a result, 4′-n-heptyl-4′-demethylharringtonine (1f, n-heptyl derivative)(I) showed the most potent cytotoxicity among the HT ester derivatives produced, with IC50 values of 9.4 nM and 0.4 μM for HL-60 and HeLa cells, resp. Interestingly, the cytotoxicity of derivative 1f against HL-60 and HeLa cells resp. was ~5 (IC50 = 50.5 nM) and ~10 times (IC50 = 4.0 μM) those of HT and ~2 (IC50 = 21.8 nM) and ~4 times (IC50 = 1.7 μM) more than homoharringtonine (HHT). These results demonstrate the potential of the derivative 1f as a lead compound against leukemia. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Application In Synthesis of tert-Butyl trichloroacetimidate
The Article related to harringtonine ester derivative antiproliferative leukemia cephalotaxus, Placeholder for records without volume info and other aspects.Application In Synthesis of tert-Butyl trichloroacetimidate
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