Development of new TAK-285 derivatives as potent EGFR/HER2 inhibitors possessing antiproliferative effects against 22RV1 and PC3 prostate carcinoma cell lines
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Son, Seohyun | - |
dc.contributor.author | Elkamhawy, Ahmed | - |
dc.contributor.author | Gul, Anam Rana | - |
dc.contributor.author | Al‐Karmalawy, Ahmed A. | - |
dc.contributor.author | Alnajjar, Radwan | - |
dc.contributor.author | Abdeen, Ahmed | - |
dc.contributor.author | Ibrahim, Samah F. | - |
dc.contributor.author | Alshammari, Saud O. | - |
dc.contributor.author | Alshammari, Qamar A. | - |
dc.contributor.author | Choi, Won Jun | - |
dc.contributor.author | Park, Tae Jung | - |
dc.contributor.author | Lee, Kyeong | - |
dc.date.accessioned | 2023-09-15T00:40:58Z | - |
dc.date.available | 2023-09-15T00:40:58Z | - |
dc.date.issued | 2023-12 | - |
dc.identifier.issn | 1475-6366 | - |
dc.identifier.issn | 1475-6374 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/67586 | - |
dc.description.abstract | Epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) protein tyrosine kinases co-expressed in various cancers such as ovarian, breast, colon, and prostate subtypes. Herein, new TAK-285 derivatives (9a–h) were synthesised, characterised, and biologically evaluated as dual EGFR/HER2 inhibitors. Compound 9f exhibited IC50 values of 2.3 nM over EGFR and 234 nM over HER2, which is 38-fold of staurosporine and 10-fold of TAK-285 over EGFR. Compound 9f also showed high selectivity profile when tested over a small kinase panel. Compounds 9a–h showed IC50 values in the range of 1.0–7.3 nM and 0.8–2.8 nM against PC3 and 22RV1 prostate carcinoma cell lines, respectively. Cell cycle analysis, apoptotic induction, molecular docking, dynamics, and MM-GBSA studies confirmed the plausible mechanism(s) of compound 9f as a potent EGFR/HER2 dual inhibitor with an effective antiproliferative action against prostate carcinoma. © 2023 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | Taylor and Francis Ltd. | - |
dc.title | Development of new TAK-285 derivatives as potent EGFR/HER2 inhibitors possessing antiproliferative effects against 22RV1 and PC3 prostate carcinoma cell lines | - |
dc.type | Article | - |
dc.identifier.doi | 10.1080/14756366.2023.2202358 | - |
dc.identifier.bibliographicCitation | Journal of Enzyme Inhibition and Medicinal Chemistry, v.38, no.1 | - |
dc.description.isOpenAccess | Y | - |
dc.identifier.wosid | 000976066100001 | - |
dc.identifier.scopusid | 2-s2.0-85153607649 | - |
dc.citation.number | 1 | - |
dc.citation.title | Journal of Enzyme Inhibition and Medicinal Chemistry | - |
dc.citation.volume | 38 | - |
dc.type.docType | Article | - |
dc.publisher.location | 영국 | - |
dc.subject.keywordAuthor | apoptosis | - |
dc.subject.keywordAuthor | chemical synthesis | - |
dc.subject.keywordAuthor | EGFR/HER2 | - |
dc.subject.keywordAuthor | kinase panel | - |
dc.subject.keywordAuthor | prostate carcinoma | - |
dc.subject.keywordPlus | BIOLOGICAL EVALUATION | - |
dc.subject.keywordPlus | LAPATINIB RESISTANCE | - |
dc.subject.keywordPlus | LUNG-CANCER | - |
dc.subject.keywordPlus | EGFR | - |
dc.subject.keywordPlus | DESIGN | - |
dc.subject.keywordPlus | MUTATION | - |
dc.subject.keywordPlus | FAMILY | - |
dc.subject.keywordPlus | KINASES | - |
dc.subject.keywordPlus | COMPLEX | - |
dc.relation.journalResearchArea | Biochemistry & Molecular Biology | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Biochemistry & Molecular Biology | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.
84, Heukseok-ro, Dongjak-gu, Seoul, Republic of Korea (06974)02-820-6194
COPYRIGHT 2019 Chung-Ang University All Rights Reserved.
Certain data included herein are derived from the © Web of Science of Clarivate Analytics. All rights reserved.
You may not copy or re-distribute this material in whole or in part without the prior written consent of Clarivate Analytics.