Synthesis and anti-proliferative activity evaluation of N3-acyl-N5-aryl-3,5-diaminoindazole analogues as anti-head and neck cancer agent

Authors
Jinho LeeJina KimVictor Sukbong HongJong-Wook Park
Department
Dept. of Immunology (면역학)
Issue Date
2014
Citation
Daru, Vol.22(1) : 4-4, 2014
ISSN
1560-8115
Abstract
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
URI
http://kumel.medlib.dsmc.or.kr/handle/2015.oak/35547
Appears in Collections:
1. Journal Papers (연구논문) > 1. School of Medicine (의과대학) > Dept. of Immunology (면역학)
Keimyung Author(s)
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