Synthesis and anti-proliferative activity evaluation of N3-acyl-N5-aryl-3,5-diaminoindazole analogues as anti-head and neck cancer agent
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- Park, Jong Wook
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- Background: Head and neck squamous cell carcinoma (HNSCC) is the 11th leading cancer by incidence
worldwide. Surgery and radiotherapy have been the major treatment for patients with HNSCC while chemotherapy
has become an important treatment option for locally advanced HNSCC. Understanding of the molecular
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.
Results: A series of N3-acyl-N5-aryl-3,5-diaminoindazoles were synthesized and their anti-proliferative 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.
Compound 9a and 9b showed more than 7-fold selectivity for AMC-HN4 and AMC-HN3, respectively.
Conclusions: N3-acyl-N5-aryl-3,5-diaminoindazole analogues can be used as hits in the development of
anticancer drug for HNSCC.
Keywords: Indazole, 3,5-diaminoindazole, Anticancer, HNSCC
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