Nam, Dong Hyuk Lee, Kwang Seob Kim, Sang Hoon Kim, Sung Min Jung, Seo Yun Chung, Sung Hyun Kim, Hyoung Ja Kim, Nam Doo Jin, Changbae Lee, Yong Sup 2024-01-21T00:01:48Z 2024-01-21T00:01:48Z 2021-09-03 2008-01-01 0960-894X https://pubs.kist.re.kr/handle/201004/133826 Calpains are involved in a variety of calcium-regulated cellular processes, such as signal transduction, cell proliferation, differentiation, and apoptosis. Excessive calpain activation contributes to serious cellular damage and has been reported in many pathological conditions. 4-Quinolinone 2-carboxamide derivatives were prepared and evaluated for mu-calpain inhibitory activities. Of the compounds synthesized, 3a and 3k, which possess a primary amide and 4-methoxyphenethyl amide at P-1' region, were found to most potently inhibit mu-calpain with IC50 values of 0.71 +/- 0.07 and 0.73 +/- 0.23 mu M, respectively. On the other hand, the incorporation of pyridine-containing amides decreased inhibitory activity. (C) 2007 Elsevier Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD Design and synthesis of 4-quinolinone 2-carboxamides as calpain inhibitors Article 10.1016/j.bmcl.2007.10.097 1 BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.18, no.1, pp.205 - 209 BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 18 1 205 209 scie scopus 000253720300034 2-s2.0-37649016170 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article calpain inhibitor stroke 4-quinolinone chromone