Chlorinated organic compounds are found in nearly every class of biomolecules. 3900-89-8, formula is C6H6BClO2, Name is (2-Chlorophenyl)boronic acid. Alkyl chlorides, as versatile building blocks in organic chemistry, are used in the preparation of alcohols, thioethers, alkenes, alkynes, esters, and Grignard reagents. Name: (2-Chlorophenyl)boronic acid.
Cheng, Bao;Zhu, Guirong;Meng, Linghua;Wu, Guolin;Chen, Qin;Ma, Shengming research published 《 Identification and optimization of biphenyl derivatives as novel tubulin inhibitors targeting colchicine-binding site overcoming multidrug resistance》, the research content is summarized as follows. Microtubule targeting agents (MTAs) are among the most successful chemotherapeutic drugs, but their efficacy is often limited by the development of multidrug resistance (MDR). Therefore, the development of novel MTAs with the ability to overcome MDR is urgently needed. In this contribution, through modification of the unsym. biaryl compounds, we discovered a novel compound dxy-1-175 with potent anti-proliferative activity against cancer cells. Mechanistic study revealed that dxy-1-175 inhibited tubulin polymerization by interacting with the colchicine-binding site of tubulin, which caused cell cycle arrest at G2/M phase. Based on the predicted binding model of dxy-1-175 with tubulin, a series of new 4-benzoylbiphenyl analogs were designed and synthesized. Among them, the hydrochloride compound 12e with improved solubility and good stability in human liver microsome, exhibited the most potent anti-proliferative activity with IC50 value in the low nanomolar range, and markedly inhibited the growth of breast cancer 4T1 xenograft in vivo. Notably, 12e effectively overcame P-gp-mediated MDR and our preliminary data suggested that 12e may not be a substrate of P-glycoprotein (P-gp). Taken together, our study reveals a novel MTA 12e targeting the colchicine-binding site with potent anticancer activity and the ability to circumvent MDR.
Name: (2-Chlorophenyl)boronic acid, 2-Chlorophenylboronic acid is a useful research compound. Its molecular formula is C6H6BClO2 and its molecular weight is 156.38 g/mol. The purity is usually 95%.
2-Chlorophenylboronic acid used in the preparation of imidazo[1,2-a]pyridine amides which has tuberculostatic activity.
2-Chlorophenylboronic acid is a diphenyl ether that can be used as a building block for the synthesis of benzodiazepine receptor ligands. It has been shown to be an efficient nucleophile, leading to the formation of carbonyl groups in the presence of halides. 2-Chlorophenylboronic acid has also been shown to inhibit p38 kinase activity and may be useful for anticancer therapy., 3900-89-8.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics