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Isatin Derived Spirocyclic Analogues with α-Methylene-γ-butyrolactone as Anticancer Agents: A Structure-Activity Relationship Study.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2016 May 26; Vol. 59 (10), pp. 5121-7. Date of Electronic Publication: 2016 Apr 26. - Publication Year :
- 2016
-
Abstract
- Design, synthesis, and evaluation of α-methylene-γ-butyrolactone analogues and their evaluation as anticancer agents is described. SAR identified a spirocyclic analogue 19 that inhibited TNFα-induced NF-κB activity, cancer cell growth and tumor growth in an ovarian cancer model. A second iteration of synthesis and screening identified 29 which inhibited cancer cell growth with low-μM potency. Our data suggest that an isatin-derived spirocyclic α-methylene-γ-butyrolactone is a suitable core for optimization to identify novel anticancer agents.<br />Competing Interests: Notes The authors declare no competing financial interest.
- Subjects :
- Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cell Line, Tumor
Cell Proliferation drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Isatin chemistry
Molecular Structure
NF-kappa B antagonists & inhibitors
NF-kappa B metabolism
Spiro Compounds chemical synthesis
Spiro Compounds chemistry
Structure-Activity Relationship
Tumor Necrosis Factor-alpha antagonists & inhibitors
Tumor Necrosis Factor-alpha metabolism
Antineoplastic Agents pharmacology
Isatin pharmacology
Spiro Compounds pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 59
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 27077228
- Full Text :
- https://doi.org/10.1021/acs.jmedchem.6b00400