Abstract
BackgroundHead 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.ResultsA 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.ConclusionsN3-acyl-N5-aryl-3,5-diaminoindazole analogues can be used as hits in the development of anticancer drug for HNSCC.
Highlights
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
A combination of radiotherapy and chemotherapy has increasingly been used for the treatment of HNSCC
Summary
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. The development and combinations of targeted therapies in different cellular pathways may be needed to fulfill the unmet needs of current HNSCC chemotherapy. Head and neck squamous cell carcinoma (HNSCC) is the 11th leading cancer by incidence worldwide [1]. Surgery and radiotherapy have been the major treatment for patients with HNSCC. Radiotherapy is used as a single treatment option in early-stage cancers and as an adjuvant treatment. A combination of radiotherapy and chemotherapy has increasingly been used for the treatment of HNSCC. Ten year follow up study of the Head and Neck trials showed that the concomitant non-
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