Abstract
We previously reported that the phenanthroindolizidine alkaloid 3 and its derivatives had markedly potent in vitro cytotoxicity. However, they had low in vivo antitumor activities and high in vivo toxicities, which was a serious problem for further development. Based on the finding that antitumor activity and toxicity could be improved by acetylation of 3, we synthesized new derivatives of 3, which possessed various acyl groups, and evaluated their antitumor activities and toxicities. We found that derivatives with sterically less bulky acyl groups had improved antitumor activities.
Keywords: Asclepiadaceae family, Ideopsis similis, alkaloids, acylated derivatives, anti-inflammatory, Meth A sarcoma, cytotoxicities, pharmacokinetic parameters, Carbonate-type derivatives, H-NMR spectra
Letters in Drug Design & Discovery
Title:Synthesis of Phenanthroindolizidine Alkaloids with an Acyloxy Group at the C3 Position and their Antitumor Activities and Toxicities
Volume: 9 Issue: 5
Author(s): Takashi Ikeda, Takashi Yaegashi, Takeshi Matsuzaki, Ryuta Yamazaki, Satoshi Ueno, Syusuke Hashimoto, Seigo Sawada
Affiliation:
Keywords: Asclepiadaceae family, Ideopsis similis, alkaloids, acylated derivatives, anti-inflammatory, Meth A sarcoma, cytotoxicities, pharmacokinetic parameters, Carbonate-type derivatives, H-NMR spectra
Abstract: We previously reported that the phenanthroindolizidine alkaloid 3 and its derivatives had markedly potent in vitro cytotoxicity. However, they had low in vivo antitumor activities and high in vivo toxicities, which was a serious problem for further development. Based on the finding that antitumor activity and toxicity could be improved by acetylation of 3, we synthesized new derivatives of 3, which possessed various acyl groups, and evaluated their antitumor activities and toxicities. We found that derivatives with sterically less bulky acyl groups had improved antitumor activities.
Export Options
About this article
Cite this article as:
Takashi Ikeda, Takashi Yaegashi, Takeshi Matsuzaki, Ryuta Yamazaki, Satoshi Ueno, Syusuke Hashimoto, Seigo Sawada , Synthesis of Phenanthroindolizidine Alkaloids with an Acyloxy Group at the C3 Position and their Antitumor Activities and Toxicities, Letters in Drug Design & Discovery 2012; 9 (5) . https://dx.doi.org/10.2174/157018012800389232
DOI https://dx.doi.org/10.2174/157018012800389232 |
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
-
Camptothecins and Lung Cancer: Improved Delivery Systems by Aerosol
Current Cancer Drug Targets Metabolic Functions of Myostatin and GDF11
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Current Perspective of Natural Alkaloid Carbazole and its Derivatives as Antitumor Agents
Anti-Cancer Agents in Medicinal Chemistry Role of PARP Inhibitors in Cancer Biology and Therapy
Current Medicinal Chemistry Mesenchymal Stem Cells: A New Generation of Therapeutic Agents as Vehicles in Gene Therapy
Current Gene Therapy Angiotensin-(1-7): A Peptide Hormone with Anti-Cancer Activity
Current Medicinal Chemistry Bioinformatics and Drug Discovery
Current Topics in Medicinal Chemistry The Therapeutic Potential of Stem Cells in Amyotrophic Lateral Sclerosis
Current Signal Transduction Therapy Neddylation Pathway as a Novel Anti-cancer Target: Mechanistic Investigation and Therapeutic Implication
Anti-Cancer Agents in Medicinal Chemistry Mechanisms Governing Lentivirus Integration Site Selection
Current Gene Therapy The Insulin-Like Growth Factor (IGF) Signaling Pathway: Strategies for Successful Therapeutic Tasks in Cancer Treatment
Current Cancer Therapy Reviews Posttranscriptional Regulation of p53 and its Targets by RNABinding Proteins
Current Molecular Medicine Molecular Modelling and QSAR in the Discovery of HIV-1 Integrase Inhibitors
Current Computer-Aided Drug Design Src Family Kinases in the Central Nervous System: Their Emerging Role in Pathophysiology of Migraine and Neuropathic Pain
Current Neuropharmacology Novel Therapeutic Strategies Against Cancer: Marine-derived Drugs May Be the Answer?
Anti-Cancer Agents in Medicinal Chemistry The Correspondence Between Magnetic Resonance Images and the Clinical and Intraoperative Status of Patients with Spinal Tumors
Current Medical Imaging Emerging Targets For Prostate Adenocarcinoma Therapy: How Molecular Biology May Drive Towards a More Tailored Approach
Current Drug Targets Revisiting Non-Cancer Drugs for Cancer Therapy
Current Topics in Medicinal Chemistry CD248: Reviewing its Role in Health and Disease
Current Drug Targets Heme Oxygenase-1 in Tumor Biology and Therapy
Current Drug Targets