Abstract
The synthesis, pharmacological properties and delivery characteristics in simulated aqueous gastric fluid of a series of symmetrical nitrogenated C2-substituted pyrrolo[2,3-f]quinolines are described. The cytotoxicity of the target molecules (5a-h) was evaluated in the human non-small lung cancer cell line NSCLCN16- L16 in vitro. One compound (5e) showed sufficient activity (IC50 = 26.4 μM) and satisfactory release characteristics from solid pharmaceutical formulations.
Keywords: Symmetrical pyrrolo[2,3-f]quinolines, Synthesis, Cytotoxicity, Drug delivery
Letters in Drug Design & Discovery
Title: Symmetrical Derivatives of C2-Substituted Pyrrolo[2,3-f]quinolines:Synthesis, Cytotoxicity and Drug Delivery Studies
Volume: 4 Issue: 2
Author(s): Andrew Tsotinis, Marilena Vlachou, Maria Gerasimopoulou, Aphrodite Eikosipentaki, Constantine Ioannidis, Anna Klouvidaki, Pandelis A. Afroudakis, Dimitri Moreau and Christos Roussakis
Affiliation:
Keywords: Symmetrical pyrrolo[2,3-f]quinolines, Synthesis, Cytotoxicity, Drug delivery
Abstract: The synthesis, pharmacological properties and delivery characteristics in simulated aqueous gastric fluid of a series of symmetrical nitrogenated C2-substituted pyrrolo[2,3-f]quinolines are described. The cytotoxicity of the target molecules (5a-h) was evaluated in the human non-small lung cancer cell line NSCLCN16- L16 in vitro. One compound (5e) showed sufficient activity (IC50 = 26.4 μM) and satisfactory release characteristics from solid pharmaceutical formulations.
Export Options
About this article
Cite this article as:
Tsotinis Andrew, Vlachou Marilena, Gerasimopoulou Maria, Eikosipentaki Aphrodite, Ioannidis Constantine, Klouvidaki Anna, Afroudakis A. Pandelis, Moreau Dimitri and Roussakis Christos, Symmetrical Derivatives of C2-Substituted Pyrrolo[2,3-f]quinolines:Synthesis, Cytotoxicity and Drug Delivery Studies, Letters in Drug Design & Discovery 2007; 4 (2) . https://dx.doi.org/10.2174/157018007779422488
DOI https://dx.doi.org/10.2174/157018007779422488 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Complexity in Clinical Trials: Blind Spots, Misleading Criteria, Winners and Losers
Clinical Cancer Drugs Therapeutic Proteins in Tumors and Targeted Therapeutic Agents for Cancer Patients
Protein & Peptide Letters Established and In-trial GPCR Families in Clinical Trials: A Review for Target Selection
Current Drug Targets Lung Cancer Prediction Using Random Forest
Recent Advances in Computer Science and Communications CCL2-CCR2 Signaling in Disease Pathogenesis
Endocrine, Metabolic & Immune Disorders - Drug Targets Ring Opening of Tetrazole via Unusual Vilsmeir-Haack Reaction Forming Novel Triazenes
Letters in Organic Chemistry 7-Azaindole Analogues as Bioactive Agents and Recent Results
Mini-Reviews in Medicinal Chemistry Resistance to Peloruside A and Laulimalide: Functional Significance of Acquired βI-tubulin Mutations at Sites Important for Drug-Tubulin Binding
Current Cancer Drug Targets Small Molecules with EGFR-TK Inhibitor Activity
Current Drug Targets A Medicinal Chemist’s Perspective Towards Structure Activity Relationship of Heterocycle Based Anticancer Agents
Current Topics in Medicinal Chemistry Sex Steroid Hormone Effects in Normal and Pathologic Conditions in Lung Physiology
Mini-Reviews in Medicinal Chemistry The Controlled Release of Drugs and Bioactive Compounds from Mesoporous Silica Nanoparticles
Current Drug Delivery Synthesis and Evaluation of Heterocycles Based Chalcone Derivatives as Antiproliferative Agents
Anti-Cancer Agents in Medicinal Chemistry Platinum Compounds: A Hope for Future Cancer Chemotherapy
Anti-Cancer Agents in Medicinal Chemistry Modulating Mitochondria-Mediated Apoptotic Cell Death through Targeting of Bcl-2 Family Proteins
Recent Patents on DNA & Gene Sequences Subcellular Trafficking in Rhabdovirus Infection and Immune Evasion: A Novel Target for Therapeutics
Infectious Disorders - Drug Targets Ionic Liquids for Topical Delivery in Cancer
Current Medicinal Chemistry <sup>99m</sup>Tc-EDDA/HYNIC-TOC is a New Opportunity in Neuroendocrine Tumors of the Lung (and in other Malignant and Benign Pulmonary Diseases)
Current Radiopharmaceuticals Potential Beneficial Effects of Garlic in Oncohematology
Mini-Reviews in Medicinal Chemistry SUBJECT INDEX TO VOLUME 1
Current Genomics