《Improved HDAC inhibition, stronger cytotoxic effect and higher selectivity against leukemias and lymphomas of novel, tricyclic vorinostat analogues》 was written by Bieszczad, Bartosz; Garbicz, Damian; Switalska, Marta; Dudek, Marta K.; Warszycki, Dawid; Wietrzyk, Joanna; Grzesiuk, Elzbieta; Mieczkowski, Adam. COA of Formula: C5H9BrO2This research focused ontricyclic vorinostat analog lymphoma leukemia HDAC inhibition cytotoxic effect; HDAC inhibitors; Vorinostat; dibenzodiazocines; histone deacetylase; hydroxamic acid; selectivity. The article conveys some information:
Histone deacetylase (HDAC) inhibitors are a class of drugs used in the cancer treatment. Here, we developed a library of 19 analogs of Vorinostat, an HDAC inhibitor used in lymphomas treatment. In Vorinostat, we replaced the hydrophobic Ph group with various tricyclic ′caps′ possessing a central, eight-membered, heterocyclic ring, and investigated the HDAC activity and cytotoxic effect on the cancer and normal cell lines. We found that 3 out of the 19 compounds, based on dibenzo[b,f]azocin-6(5H)-one, 11,12-dihydrodibenzo[b,f]azocin-6(5H)-one, and benzo[b]naphtho[2,3-f][1,5]diazocine-6,14(5H,13H)-dione scaffolds, showed better HDACs inhibition than the referenced Vorinostat. In leukemic cell line MV4-11 and in the lymphoma cell line Daudi, three compounds showed lower IC50 values than Vorinostat. These compounds had higher activity and selectivity against MV4-11 and Daudi cell lines than reference Vorinostat. We also observed a strong correlation between HDACs inhibition and the cytotoxic effect. Cell lines derived from solid tumors: A549 (lung carcinoma) and MCF-7 (breast adenocarcinoma) as well as reference BALB/3T3 (normal murine fibroblasts) were less susceptible to compounds tested. Developed derivatives show improved properties than Vorinostat, thus they could be considered as possible agents for leukemia and lymphoma treatment. The experimental part of the paper was very detailed, including the reaction process of Ethyl 3-bromopropanoate(cas: 539-74-2COA of Formula: C5H9BrO2)
Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. COA of Formula: C5H9BrO2 In contrast, terrestrial plants account only for a few bromine-containing compounds.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary