Abstract
CuI facilitated the intramolecular cyclization of 8-alkynyl substituted 2,3-dihydroquinolin-4(1H)-ones leading to 5-subtituted 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-1-ones via intramolecular C-N bond forming reaction. Some of the synthesized compounds have shown encouraging inhibition of Sir 2 protein (a yeast homolog of mammalian SIRT1) when tested using a yeast cell based assay. A representative compound showed dose dependent inhibition of yeast Sir 2 (IC50 = 30.09 µM) and cell growth inhibition properties when tested against different cancer cell lines. It’s in silico interactions with sirtuins are presented.
Keywords: Alkyne, CuI, Cyclization, Docking, Pyrroloquinolines, Sirtuins.
Letters in Drug Design & Discovery
Title:Cu-mediated synthesis of 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-1-ones as potential inhibitors of sirtuins
Volume: 11 Issue: 2
Author(s): Sreerama Srinivas Rao, Dandela Rambabu, Mohosin Layek, Kummari Lalith Kumar, Mandava Venkata Basaveswara Rao, Devyani Haldar and Manojit Pal
Affiliation:
Keywords: Alkyne, CuI, Cyclization, Docking, Pyrroloquinolines, Sirtuins.
Abstract: CuI facilitated the intramolecular cyclization of 8-alkynyl substituted 2,3-dihydroquinolin-4(1H)-ones leading to 5-subtituted 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-1-ones via intramolecular C-N bond forming reaction. Some of the synthesized compounds have shown encouraging inhibition of Sir 2 protein (a yeast homolog of mammalian SIRT1) when tested using a yeast cell based assay. A representative compound showed dose dependent inhibition of yeast Sir 2 (IC50 = 30.09 µM) and cell growth inhibition properties when tested against different cancer cell lines. It’s in silico interactions with sirtuins are presented.
Export Options
About this article
Cite this article as:
Srinivas Rao Sreerama, Rambabu Dandela, Layek Mohosin, Lalith Kumar Kummari, Venkata Basaveswara Rao Mandava, Haldar Devyani and Pal Manojit, Cu-mediated synthesis of 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-1-ones as potential inhibitors of sirtuins, Letters in Drug Design & Discovery 2014; 11 (2) . https://dx.doi.org/10.2174/15701808113109990065
DOI https://dx.doi.org/10.2174/15701808113109990065 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
Related Journals
Related Books
- 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
-
Targeting Tumor Angiogenesis in Gastrointestinal Malignancies
Current Angiogenesis (Discontinued) Advances in the Development of Class I Phosphoinositide 3-Kinase (PI3K) Inhibitors
Current Topics in Medicinal Chemistry Epigallocatechin-3-Gallate Prevents Autoimmune-Associated Down- Regulation of p21 in Salivary Gland Cells Through a p53-Independent Pathway
Inflammation & Allergy - Drug Targets (Discontinued) Physcion and Physcion 8-O-β-D-glucopyranoside: Natural Anthraquinones with Potential Anticancer Activities
Current Drug Targets DNMT Inhibitors in Cancer, Current Treatments and Future Promising Approach: Inhibition of Specific DNMT-Including Complexes
Epigenetic Diagnosis & Therapy (Discontinued) Linking Inflammation to Cell Cycle Progression
Current Pharmaceutical Design Preclinical Drug Discovery in Colorectal Cancer: A Focus on Natural Compounds
Current Drug Targets Pharmacological Aspects and Potential Use of Phloretin: A Systemic Review
Mini-Reviews in Medicinal Chemistry Notch Signalling Pathways and Their Importance in the Treatment of Cancers
Current Drug Targets Immunotherapeutic Options for Pediatric Malignancies
Current Immunology Reviews (Discontinued) An Innovative Fluorescent Semi-quantitative Methylation-specific PCR Method for the Determination of MGMT Promoter Methylation is Reflecting Intra-tumor Heterogeneity
Current Cancer Drug Targets Base-Modified Nucleosides as Chemotherapeutic Agents: Past and Future
Current Topics in Medicinal Chemistry Signaling Transduction Network Mediated by Tumor Suppressor/Susceptibility Genes in NPC
Current Genomics The Evaluation of Potential Cytotoxic Effect of Different Proton Pump Inhibitors on Different Human Cancer Cell Lines
Anti-Cancer Agents in Medicinal Chemistry Repurposing Non-Antimicrobial Drugs and Clinical Molecules to Treat Bacterial Infections
Current Pharmaceutical Design The Interplay between the Gut Immune System and Microbiota in Health and Disease: Nutraceutical Intervention for Restoring Intestinal Homeostasis
Current Pharmaceutical Design Adenovirus-based Immunotherapy for Prostate Cancer
Current Cancer Therapy Reviews Oxidative Stress and its Clinical Consequences: Relationship between Diabetes and Cancer
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Recent Developments in Female Hormonal Contraception
Current Women`s Health Reviews Pomegranate, its Components, and Modern Deliverable Formulations as Potential Botanicals in the Prevention and Treatment of Various Cancers
Current Drug Delivery