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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LEE JINHO; KIM JINA; HONG VICTOR SUKBONG; PARK JONG WOOK

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Journal Paper

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Journal: DARU Journal of Pharmaceutical Sciences Year:2014 | Volume:22 | Issue:1 Page(s): 1-9

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Title

SYNTHESIS AND ANTI-PROLIFERATIVE ACTIVITY EVALUATION OF N3-ACYL-N5-ARYL-3, 5-DIAMINOINDAZOLE ANALOGUES AS ANTI-HEAD AND NECK CANCER AGENT

Author(s)

LEE JINHO | KIM JINA | HONG VICTOR SUKBONG | PARK JONG WOOK | Issue Writer Certificate

Keywords

INDAZOLE

5-DIAMINOINDAZOLE

ANTICANCER

HNSCC

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.

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APA: Copy

LEE, JINHO, KIM, JINA, HONG, VICTOR SUKBONG, & PARK, JONG WOOK. (2014). SYNTHESIS AND ANTI-PROLIFERATIVE ACTIVITY EVALUATION OF N3-ACYL-N5-ARYL-3, 5-DIAMINOINDAZOLE ANALOGUES AS ANTI-HEAD AND NECK CANCER AGENT. DARU JOURNAL OF PHARMACEUTICAL SCIENCE, 22(1), 1-9. SID. https://sid.ir/paper/275721/en

Vancouver: Copy

LEE JINHO, KIM JINA, HONG VICTOR SUKBONG, PARK JONG WOOK. SYNTHESIS AND ANTI-PROLIFERATIVE ACTIVITY EVALUATION OF N3-ACYL-N5-ARYL-3, 5-DIAMINOINDAZOLE ANALOGUES AS ANTI-HEAD AND NECK CANCER AGENT. DARU JOURNAL OF PHARMACEUTICAL SCIENCE[Internet]. 2014;22(1):1-9. Available from: https://sid.ir/paper/275721/en

IEEE: Copy

JINHO LEE, JINA KIM, VICTOR SUKBONG HONG, and JONG WOOK PARK, “SYNTHESIS AND ANTI-PROLIFERATIVE ACTIVITY EVALUATION OF N3-ACYL-N5-ARYL-3, 5-DIAMINOINDAZOLE ANALOGUES AS ANTI-HEAD AND NECK CANCER AGENT,” DARU JOURNAL OF PHARMACEUTICAL SCIENCE, vol. 22, no. 1, pp. 1–9, 2014, [Online]. Available: https://sid.ir/paper/275721/en

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