Abstract
To search for novel anticancer agents, we designed and synthesized a series of new triazolyl berberine derivatives. The evaluation of all the synthesized compounds and their anticancer activities against a panel of four human cancer cell lines including MCF-7 (breast), MCF-7/ADR (breast), SW-1990 (pancreatic), SMMC-7721 (liver) and the noncancer cell line HUVEC (human umbilical vein endothelial cell). The results showed that most of the compounds displayed better anticancer activities against MCF-7 and SMMC-7721 compared with berberine. Among these derivatives, compounds 5p and 5a exhibited the most potent inhibitory activities against the SMMC-7721 and SW-1990 cell lines with IC50 values of 14.861 ± 2.4 µM and 16.798 ± 3.4 µM. Furthermore, compounds 5p, 5a and 5n exhibited much better selectivity toward the normal cell line HUVEC than berberine.
Keywords: Anticancer, berberine, click chemistry, structure-activity relationship.
Anti-Cancer Agents in Medicinal Chemistry
Title:Novel Triazolyl Berberine Derivatives Prepared via CuAAC Click Chemistry: Synthesis, Anticancer Activity and Structure-Activity Relationships
Volume: 15 Issue: 1
Author(s): Xin Jin, Lan Yan, Hong-jiao Li, Rui-Lian Wang, Zhen-Lin Hu, Yuan-Ying Jiang, Yong-Bing Cao, Tian-Hua Yan and Qing-Yan Sun
Affiliation:
Keywords: Anticancer, berberine, click chemistry, structure-activity relationship.
Abstract: To search for novel anticancer agents, we designed and synthesized a series of new triazolyl berberine derivatives. The evaluation of all the synthesized compounds and their anticancer activities against a panel of four human cancer cell lines including MCF-7 (breast), MCF-7/ADR (breast), SW-1990 (pancreatic), SMMC-7721 (liver) and the noncancer cell line HUVEC (human umbilical vein endothelial cell). The results showed that most of the compounds displayed better anticancer activities against MCF-7 and SMMC-7721 compared with berberine. Among these derivatives, compounds 5p and 5a exhibited the most potent inhibitory activities against the SMMC-7721 and SW-1990 cell lines with IC50 values of 14.861 ± 2.4 µM and 16.798 ± 3.4 µM. Furthermore, compounds 5p, 5a and 5n exhibited much better selectivity toward the normal cell line HUVEC than berberine.
Export Options
About this article
Cite this article as:
Jin Xin, Yan Lan, Li Hong-jiao, Wang Rui-Lian, Hu Zhen-Lin, Jiang Yuan-Ying, Cao Yong-Bing, Yan Tian-Hua and Sun Qing-Yan, Novel Triazolyl Berberine Derivatives Prepared via CuAAC Click Chemistry: Synthesis, Anticancer Activity and Structure-Activity Relationships, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (1) . https://dx.doi.org/10.2174/1871520614666141203142012
DOI https://dx.doi.org/10.2174/1871520614666141203142012 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
- 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
-
MicroRNA: Implications for Alzheimer Disease and other Human CNS Disorders
Current Genomics Female Infertility and Assisted Reproduction: Impact of Oxidative Stress-- An Update
Current Women`s Health Reviews Current Issues in Tumor Immunology
Current Bioinformatics Indole Derivatives as Anticancer Agents for Breast Cancer Therapy: A Review
Anti-Cancer Agents in Medicinal Chemistry Looking out for Cancer Stem Cells’ Properties: The Value-Driving Role of CD44 for Personalized Medicines
Current Cancer Drug Targets Targeting Poly (ADP) Ribose Polymerase I (PARP-1) and PARP-1 Interacting Proteins for Cancer Treatment
Anti-Cancer Agents in Medicinal Chemistry Topical Lipid Based Drug Delivery Systems for Skin Diseases: A Review
Current Drug Therapy Copper Complexes as Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Pharmacogenetics of Irinotecan Disposition and Toxicity: A Review
Current Clinical Pharmacology Novel Targets for Apoptosis Modulation: BAG3 Protein and Other Co- Chaperones
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Meta-heuristic Techniques to Train Artificial Neural Networks for Medical Image Classification: A Review
Recent Advances in Computer Science and Communications Intestinal Immunomodulation. Role of Regulative Peptides and Promising Pharmacological Activities
Current Pharmaceutical Design Antiangiogenic Therapy
Current Pharmaceutical Design New Ways to Improve Breast Cancer Therapy Targeting Specific Molecular Pathways
Current Cancer Therapy Reviews Intracellular Bioinorganic Chemistry and Cross Talk Among Different -Omics
Current Topics in Medicinal Chemistry Impact of RET Screening on the Management of Multiple Endocrine Neoplasia Type 2A: 10 Years Experience and Follow-Up in Three Families
Endocrine, Metabolic & Immune Disorders - Drug Targets Overview of Prostate Biomarkers as Potential Targets for Immunotherapy
Current Cancer Therapy Reviews The Protein-Protein Interaction-Mediated Inactivation of PTEN
Current Molecular Medicine Oral Cavity-Associated Immune System: What is New?
Current Immunology Reviews (Discontinued) Classical to Current Approach for Treatment of Psoriasis: A Review
Endocrine, Metabolic & Immune Disorders - Drug Targets