Synthesis and anti-proliferative activity evaluation of N3-acyl-N5-aryl-3,5-diaminoindazole analogues as anti-head and neck cancer agent was written by Lee, Jinho;Kim, Jina;Hong, Victor Sukbong;Park, Jong-Wook. And the article was included in Daru, Journal of Pharmaceutical Sciences in 2014.Product Details of 1130165-74-0 This article mentions the following:
Head and neck squamous cell carcinoma (HNSCC) is the 11th leading cancer by incidence worldwide. Surgery and radiotherapy were the major treatment for patients with HNSCC while chemotherapy become an important treatment option for locally advanced HNSCC. Understanding of the mol. mechanisms underlying HNSCC impelled the development of targeted therapeutic agents. The development and combinations of targeted therapies in different cellular pathways may be needed to fulfill the unmet needs of current HNSCC chemotherapy. A series of N3-acyl-N5-aryl-3,5-diaminoindazoles were synthesized and their antiproliferative activities were evaluated against human cancer cell lines, Caki, A549, AMC-HN1, AMC-HN3, AMC-HN4, AMC-HN6, and SNU449. The cellular selectivity of compound was obtained by the modification of substituent at N5-aryl group of 3,5-diaminoindazole. The compounds 2-(4-ethoxyphenyl)-N-{5-[2-fluoro-4-(morpholine-4-carbonyl)phenylamino]-1H-indazol-3-yl}acetamide and 2-(4-ethoxyphenyl)-N-{5-[2-fluoro-4-(4-methylpiperazine-1-carbonyl)phenylamino]-1H-indazol-3-yl}acetamide showed more than 7-fold selectivity for AMC-HN4 and AMC-HN3, resp. 3-Acylamino-N-arylaminoindazole analogs were used as hits in the development of anticancer drug for HNSCC. In the experiment, the researchers used many compounds, for example, Ethyl 4-bromo-3-fluorobenzoate (cas: 1130165-74-0Product Details of 1130165-74-0).
Ethyl 4-bromo-3-fluorobenzoate (cas: 1130165-74-0) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents. Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.Product Details of 1130165-74-0
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary