El-Damasy, Ashraf Kareem Cho, Nam-Chul Kang, Soon Bang Pae, Ae Nim Keum, Gyochang 2024-01-20T07:02:46Z 2024-01-20T07:02:46Z 2021-09-05 2015-05-15 0960-894X https://pubs.kist.re.kr/handle/201004/125441 A series of novel picolinamide based benzothiazoles (17 final compounds), targeting both wild-type and the most resistant T315I mutant of Bcr-Abl kinase, has been designed and synthesized. Moreover, a selected array (8 compounds) was evaluated for its antiproliferative activity over a panel of 60 cancer cell lines. Compound 5l was the most potent derivative against both native and T315I mutant ABL with IC50 values of 18.2 and 39.9 nM, respectively, and showed highly selective inhibitory activity (89.8%) towards the Bcr-Abl dependent leukemia cell (K-562) at 10 mu M concentration. Significance of C6-oxypicolinamide moiety and SAR study for the C2 aliphatic side chain of benzothiazole are discussed in detail. (C) 2015 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. CHRONIC MYELOID-LEUKEMIA CHRONIC MYELOGENOUS LEUKEMIA NATIONAL-CANCER-INSTITUTE REGORAFENIB BAY 73-4506 BCR-ABL MULTIKINASE INHIBITOR ANTICANCER DRUG T315I MUTANT CELL-LINES DISCOVERY ABL kinase inhibitory and antiproliferative activity of novel picolinamide based benzothiazoles Article 10.1016/j.bmcl.2015.03.067 1 Bioorganic & Medicinal Chemistry Letters, v.25, no.10, pp.2162 - 2168 Bioorganic & Medicinal Chemistry Letters 25 10 2162 2168 scie scopus 000353526300028 2-s2.0-84937759505 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article CHRONIC MYELOID-LEUKEMIA CHRONIC MYELOGENOUS LEUKEMIA NATIONAL-CANCER-INSTITUTE REGORAFENIB BAY 73-4506 BCR-ABL MULTIKINASE INHIBITOR ANTICANCER DRUG T315I MUTANT CELL-LINES DISCOVERY Chronic myelogenous leukemia ABL kinase T315I mutant Picolinamide Benzothiazole Antiproliferative