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Discovery of 6-chloro-2-(propylthio)-8,9-dihydro-7H-purines containing a carboxamide moiety as potential selective anti-lung cancer agents.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2018 May 10; Vol. 151, pp. 327-338. Date of Electronic Publication: 2018 Apr 03. - Publication Year :
- 2018
-
Abstract
- A new series of 6-chloro-2-(propylthio)-8,9-dihydro-7H-purine-8-caboxamide derivatives were designed, synthesized, and further evaluated for their antiproliferative activities on four human cancer cell lines (A549, MGC803, PC-3 and TE-1). The structure-activity relationships (SARs) studies were conducted through the variation in the two regions, which including position 8 and 9, of purine core. One of the compounds, 8, containing a terminal piperazine appendage with a carboxamide moiety at position 8 and phenyl group at position 9 of 6-chloro-8,9-dihydro-7H-purine core, showed the most potent antiproliferative activity and good selectivity between cancer and normal cells (IC <subscript>50</subscript> values of 2.80 μM against A549 and 303.03 μM against GES-1, respectively). In addition, compound 8 could inhibit the colony formation and migration of A549 cells in a concentration-dependent manner, as well as induce the apoptosis possibly through the intrinsic pathway.<br /> (Copyright © 2018 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Apoptosis drug effects
Cell Line, Tumor
Cell Movement drug effects
Cell Proliferation drug effects
Drug Discovery
Drug Screening Assays, Antitumor
Halogenation
Humans
Lung Neoplasms pathology
Neoplasm Invasiveness pathology
Neoplasm Invasiveness prevention & control
Neoplasms drug therapy
Neoplasms pathology
Structure-Activity Relationship
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Lung Neoplasms drug therapy
Purines chemistry
Purines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 151
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 29635165
- Full Text :
- https://doi.org/10.1016/j.ejmech.2018.03.084