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Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2013 Dec 01; Vol. 21 (23), pp. 7343-56. Date of Electronic Publication: 2013 Oct 01. - Publication Year :
- 2013
-
Abstract
- Derivatives with scaffolds of 1,3,5-tri-substituted pyrazoline and 1,3,4,5-tetra-substituted pyrazoline were synthesized and tested for their inhibitory effects versus the p53(+/+) HCT116 and p53(-/-) H1299 human tumor cell lines. Several compounds were active against the two cell lines displaying IC50 values in the low micromolar range with a clearly more pronounced effect on the p53(+/+) HCT116 cells. The compound class shows excellent developability due to the modular synthesis, allowing independent optimization of all three to four key substituents to improve the properties of the molecules.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)
- Subjects :
- Cell Line, Tumor
Gene Deletion
Gene Expression Regulation, Neoplastic
Humans
Neoplasms genetics
Structure-Activity Relationship
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Growth Inhibitors chemistry
Growth Inhibitors pharmacology
Neoplasms drug therapy
Tumor Suppressor Protein p53 genetics
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 21
- Issue :
- 23
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 24139845
- Full Text :
- https://doi.org/10.1016/j.bmc.2013.09.055