Novel 3-arylethynyl-substituted thieno[3,4-b]pyrazine derivatives as human transglutaminase 2 inhibitors

Nayeon Kim; Se Hun Kwak; Seon Hyeong Lee; Vinayak Juvekar; Byung Il Lee; Hee Chul Ahn; Soo Youl Kim; Young Dae Gong

doi:10.1039/c4ob00179f

Novel 3-arylethynyl-substituted thieno[3,4-b]pyrazine derivatives as human transglutaminase 2 inhibitors

Nayeon Kim
, Se Hun Kwak
, Seon Hyeong Lee
, Vinayak Juvekar
, Byung Il Lee
, Hee Chul Ahn
, Soo Youl Kim
, Young Dae Gong

Department of Pharmacy

Dongguk University
National Cancer Center Korea

Research output: Contribution to journal › Article › peer-review

7 Scopus citations

Abstract

In the process of optimization, we developed a novel core skeleton of thieno[3,4-b]pyrazine viaGK-13. The derivatives synthesized were shown to inhibit TGase 2 activity in cancer cells. Some of the hit compounds such as the arylethynyl group-coupled thieno[3,4-b]pyrazine derivatives were shown to exhibit promising activity for use as potential therapeutic small-molecules in renal cancer by inhibiting TGase 2 activity. This journal is

Original language	English
Pages (from-to)	4932-4940
Number of pages	9
Journal	Organic and Biomolecular Chemistry
Volume	12
Issue number	27
DOIs	https://doi.org/10.1039/c4ob00179f
State	Published - 21 Jul 2014

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title = "Novel 3-arylethynyl-substituted thieno[3,4-b]pyrazine derivatives as human transglutaminase 2 inhibitors",

abstract = "In the process of optimization, we developed a novel core skeleton of thieno[3,4-b]pyrazine viaGK-13. The derivatives synthesized were shown to inhibit TGase 2 activity in cancer cells. Some of the hit compounds such as the arylethynyl group-coupled thieno[3,4-b]pyrazine derivatives were shown to exhibit promising activity for use as potential therapeutic small-molecules in renal cancer by inhibiting TGase 2 activity. This journal is",

author = "Nayeon Kim and Kwak, \{Se Hun\} and Lee, \{Seon Hyeong\} and Vinayak Juvekar and Lee, \{Byung Il\} and Ahn, \{Hee Chul\} and Kim, \{Soo Youl\} and Gong, \{Young Dae\}",

year = "2014",

month = jul,

day = "21",

doi = "10.1039/c4ob00179f",

language = "English",

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T1 - Novel 3-arylethynyl-substituted thieno[3,4-b]pyrazine derivatives as human transglutaminase 2 inhibitors

AU - Kim, Nayeon

AU - Kwak, Se Hun

AU - Lee, Seon Hyeong

AU - Juvekar, Vinayak

AU - Lee, Byung Il

AU - Ahn, Hee Chul

AU - Kim, Soo Youl

AU - Gong, Young Dae

PY - 2014/7/21

Y1 - 2014/7/21

N2 - In the process of optimization, we developed a novel core skeleton of thieno[3,4-b]pyrazine viaGK-13. The derivatives synthesized were shown to inhibit TGase 2 activity in cancer cells. Some of the hit compounds such as the arylethynyl group-coupled thieno[3,4-b]pyrazine derivatives were shown to exhibit promising activity for use as potential therapeutic small-molecules in renal cancer by inhibiting TGase 2 activity. This journal is

AB - In the process of optimization, we developed a novel core skeleton of thieno[3,4-b]pyrazine viaGK-13. The derivatives synthesized were shown to inhibit TGase 2 activity in cancer cells. Some of the hit compounds such as the arylethynyl group-coupled thieno[3,4-b]pyrazine derivatives were shown to exhibit promising activity for use as potential therapeutic small-molecules in renal cancer by inhibiting TGase 2 activity. This journal is

UR - https://www.scopus.com/pages/publications/84902789247

U2 - 10.1039/c4ob00179f

DO - 10.1039/c4ob00179f

M3 - Article

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SN - 1477-0520

VL - 12

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EP - 4940

JO - Organic and Biomolecular Chemistry

JF - Organic and Biomolecular Chemistry

IS - 27

ER -

Novel 3-arylethynyl-substituted thieno[3,4-b]pyrazine derivatives as human transglutaminase 2 inhibitors

Abstract

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