Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 110-52-1, is researched, SMILESS is BrCCCCBr, Molecular C4H8Br2Journal, Article, Bioorganic & Medicinal Chemistry Letters called Design, synthesis, and biological evaluation of phenyl thiazole-based AR-V7 degraders, Author is Bhumireddy, Archana; Bandaru, N. V. M. Rao; Raghurami Reddy, B.; Gore, Suraj T.; Mukherjee, Subhendu; Balasubramanian, Wesley Roy; Sumanth Kumar, V.; Alapati, Krishna Satya; Venkata Gowri Chandra Sekhar, Kondapalli; Nellore, Kavitha; Abbineni, Chandrasekhar; Samajdar, Susanta, the main research direction is phenyl thiazole ligand binding domain ARV7 degrader; 22Rv1; AR-V7; CRPC; Degrader; PROTAC.SDS of cas: 110-52-1.
Multiple Splice variants of AR have been reported in the past few years. These splice variants are upregulated in most cases of CRPC resulting in poor prognosis. Most of these variants lack the ligand binding domain (LBD) but still bind to DNA resulting in constitutive activation of downstream targets. The AR-V7 splice variant has been characterized extensively and current clin. trials in CRPC are exploring the use of AR-V7 as a biomarker. New therapeutic mols. that selectively target AR-V7 are also being explored. However, there is a dearth of information available on the selectivity, phenotypic responses in AR-V7 dependent cell lines and pharmacokinetic properties of such mols. Using our proprietary computational algorithms and rational SAR optimization, we have developed a potent and selective AR-V7 degrader from a known AR DNA binding domain (DBD) binder. This mol. effectively degraded AR-V7 in a CRPC cell line and demonstrated good oral bioavailability in mouse PK studies. This tool compound can be used to evaluate the pharmacol. effects of AR-V7 degraders. Further exploration of SAR can be pursued to develop more optimized lead compounds
As far as I know, this compound(110-52-1)SDS of cas: 110-52-1 can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles