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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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Affiliated Author(s)
박종욱
Alternative Author(s)
Park, Jong Wook
Journal Title
Daru
ISSN
1560-8115
Issued Date
2014
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
Department
Dept. of Immunology (면역학)
Publisher
School of Medicine
Citation
Jinho Lee et al. (2014). Synthesis and anti-proliferative activity evaluation of N3-acyl-N5-aryl-3,5-diaminoindazole analogues as anti-head and neck cancer agent. Daru, 22(1), 4–4. doi: 10.1186/2008-2231-22-4
Type
Article
ISSN
1560-8115
DOI
10.1186/2008-2231-22-4
URI
https://kumel.medlib.dsmc.or.kr/handle/2015.oak/35547
Appears in Collections:
1. School of Medicine (의과대학) > Dept. of Immunology (면역학)
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