23738-81-0Relevant academic research and scientific papers
Histone Deacetylase 2 (HDAC2) Inhibitors Containing Boron
Kavianpour, Poya,Gemmell, Madeleine C. M.,Kahlert, Jan U.,Rendina, Louis M.
, p. 2786 - 2791 (2020/06/25)
Histone deacetylase enzymes (HDACs) are responsible for the global silencing of tumour-suppressor genes. Treatment with a histone deacetylase inhibitor (HDACi) can reverse this process and restore normal cell function. Herein, we report a small series of boron-based (boronic acid, boronate ester and closo-1,2-carborane) HDAC2 inhibitors with IC50 values in the nanomolar range. The boronate ester 4 b was the most potent compound assessed in this study (IC50=40.6±1.5 nM), followed closely by the 1,2-closo-carborane (IC50=42.9±1.5 nM). Compound 4 b exceeds the potency of the related gold-standard HDAC pan-inhibitor vorinostat (1) toward this particular HDAC isoform.
Thermal curing of novel carborane-containing phenylethynyl terminated imide oligomers
Yue, Jie,Li, Yuntao,Li, Hui,Zhao, Yan,Zhao, Chunxia,Wang, Xiangyu
, p. 98010 - 98019 (2015/12/04)
A novel carborane-containing phenylethynyl terminated imide compound (Carb-PEPA) as a modifier for fluorinated phenylethynyl terminated imide oligomer (AFR-PEPA) was synthesized and characterized by FT-IR and 1H-NMR. The resin systems consisting of Carb-PEPA and AFR-PEPA (AFR-PEPA-Carb) were prepared with different weight fractions of Carb-PEPA. The thermal curing kinetics and thermal stability of the imide compound and resultant resin systems were analyzed by using DSC and TGA respectively. The relevant kinetic data were determined by a Kissinger method. The results show that the glass transition temperatures (Tg) of the cured resin systems increase with the addition of Carb-PEPA. The imide system containing 20 wt% Carb-PEPA (AFR-PEPA-Carb-20) exhibits the highest Tg of 389.5 °C due to the high steric hindrance of carborane. The char yield of the resin was also increased with the introduction of the carborane structure in the system. The kinetic data indicate that AFR-PEPA/Carb-PEPA imide blends have higher activation energy E and frequency factor A than AFR-PEPA imide oligomers.
Tumour-targetted Boranes. Part 3. Synthesis of Carbamate-linked Nitroimidazolyl Carboranes Designed for Boron Neutron Capture Therapy of Cancer
Scobie, Martin,Threadgill, Michael D.
, p. 2059 - 2064 (2007/10/02)
Carboranes targetted to specific tumour tissues are important for boron neutron capture therapy of cancer (BNCT).Carbamoylation of 2-ethoxy>ethanol 5 and 1-(chloromethyl-2-(nitroimidazol-1-yl)ethanol 6 with carboran-1-yl isocyanate (generated in situ by a Curtius rearrangement of carborane-1-carbonyl azide) gave the corresponding carbamate-linked nitroimidazolylcarboranes 16 and 17.A similar reaction of 4-carboranylphenyl isocyanate with 6 afforded the corresponding carbamate 24.
