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Targeting tyrosine kinase: Development of acridone - pyrrole - oxindole hybrids against human breast cancer.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2019 Jan 01; Vol. 29 (1), pp. 32-35. Date of Electronic Publication: 2018 Nov 10. - Publication Year :
- 2019
-
Abstract
- Based on the molecular modelling studies, a rational modification of the lead molecule was made to develop highly potent compounds showing anti-cancer activity against human breast cancer cell lines MCF 7, MDA-MB-468 and T-47D. The most potent compounds have Log P and total polar surface area 4.4-5.4 and 59.8 Å, respectively and they also exhibited promising ADME profile.<br /> (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- Subjects :
- Acridones chemical synthesis
Acridones chemistry
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Breast Neoplasms metabolism
Breast Neoplasms pathology
Cell Line, Tumor
Cell Proliferation drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Female
Humans
MCF-7 Cells
Models, Molecular
Molecular Structure
Oxindoles chemical synthesis
Oxindoles chemistry
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors chemistry
Protein-Tyrosine Kinases metabolism
Pyrroles chemical synthesis
Pyrroles chemistry
Structure-Activity Relationship
Acridones pharmacology
Antineoplastic Agents pharmacology
Breast Neoplasms drug therapy
Oxindoles pharmacology
Protein Kinase Inhibitors pharmacology
Protein-Tyrosine Kinases antagonists & inhibitors
Pyrroles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 29
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 30446310
- Full Text :
- https://doi.org/10.1016/j.bmcl.2018.11.021