55116-09-1Relevant articles and documents
Facile and efficient route to prepare luminescent terbium containing covalently anchored hybrids equipped with molecular bridge
Sui, Yu-Long,Yan, Bing,Wang, Qian-Ming
, p. 193 - 201 (2006)
A kind of monomer (abbreviated as BrBAA-APES) was prepared by modifying 2-bromophenylacetic acid (BrBAA) with a coupling agent (3-aminopropyl) triethoxysilane (APES). Then it was used to coordinate to Tb3+ and to react with tetraethoxysilane (T
Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor
Jung, Hui Jin,Nam, Eun Hye,Park, Jin Young,Ghosh, Prithwish,Kim, In Su
supporting information, (2021/02/26)
Fibroblast activation protein (FAP) belongs to the family of prolyl-specific serine proteases and displays both exopeptidase and endopeptidase activities. FAP expression is undetectable in most normal adult tissues, but is greatly upregulated in sites of tissue remodeling, which include fibrosis, inflammation and cancer. Due to its restricted expression pattern and dual enzymatic activities, FAP inhibition is investigated as a therapeutic option for several diseases. In the present study, we described the structure–activity relationship of several synthesized compounds against DPPIV and prolyl oligopeptidase (PREP). In particular, BR102910 (compound 24) showed nanomolar potency and high selectivity. Moreover, the in vivo FAP inhibition study of BR102910 (compound 24) using C57BL/6J mice demonstrated exceptional profiles and satisfactory FAP inhibition efficacy. Based on excellent in vitro and in vivo profiles, the potential of BR102910 (compound 24) as a lead candidate for the treatment of type 2 diabetes is considered.
Quantitative activity-activity relationship (QAAR) driven design to develop hydroxamate derivatives of pentanoic acids as selective HDAC8 inhibitors: synthesis, biological evaluation and binding mode of interaction studies
Adhikari, Nilanjan,Amin, Sk. Abdul,Das, Sanjib,Ghosh, Balaram,Jha, Tarun,Routholla, Ganesh,Trivedi, Prakruti,Vijayasarathi, Dhanya
, p. 17149 - 17162 (2021/10/04)
Histone deacetylase 8 (HDAC8) has been implicated as a potential drug target of many diseases including cancer. HDAC8 isoform selectivity over other class-I HDACs is a major concern nowadays. In this work, a series of pentanoic acid based hydroxamates wit
Palladium-Catalyzed 2-(Neopentylsulfinyl)aniline Directed C–H Acetoxylation and Alkenylation of Arylacetamides
Barysevich, Maryia V.,Laktsevich-Iskryk, Marharyta V.,Krech, Anastasiya V.,Zhabinskii, Vladimir N.,Khripach, Vladimir A.,Hurski, Alaksiej L.
supporting information, p. 937 - 943 (2020/02/25)
The 2-(neopentylsulfinyl)aniline directing group that promotes rapid palladium-catalyzed C–H acetoxylation and alkenylation of arylacetamides has been developed. The acetoxylation reaches completion within only 40 min at 100 °C and leads to the bis-functionalized products. Alternatively, the reaction can be carried out at room temperature, which is beneficial for sensitive substrates. For the alkenylation, we have developed a protocol in which easily available 1-substituted cyclopropanols were employed as equivalents of vinyl ketones.