Abstract
A series of 14 N-acyl-hydrazones L-serine derivatives have been synthesized and evaluated for their in vitro antitumoral activities against four neoplastic cancer cells: HL-60 (leukemia), MDA-MB-435 (melanoma), HCT-8 (colon) and SF-295 (nervous system). Five compounds (3g, 3h, 3i, 3k and 3n) were considered active against at least two cancer cell lines, with more than 90% of growth inhibition. Compound 3h, with IC50 of 2.04 μg/mL, seems to be moderately selective to HCT-8 and can be considered in further studies aiming new prototypes for a lead molecule against colon cancer.
Keywords: L-serine, Hydrazones, Cancer, Conagenin, Lymphokines, Antitumoral Evaluation, Streptomyces roseosporus, ceramidase inhibitors, apoptosis, tumor suppressor lipid, sphingosine kinase inhibitor, Pharmacological Studies, Melting points, IC50
Letters in Drug Design & Discovery
Title: Synthesis and Antitumoral Evaluation of Benzyl (1S)-2-[2-(monosubstituted-benzylidene)hydrazino]-1-(hydroxymethyl)-2-oxoethylcarbamate
Volume: 9 Issue: 3
Author(s): Raquel Carvalho Montenegro, Leticia Veras Costa Lotufo, Manoel Odorico de Moraes, Claudia do O Pessoa, Felipe Augusto Rocha Rodrigues, Alessandra Campbell Pinheiro, Thais Cristina Mendonça Nogueira and Marcus Vinicius Nora de Souza
Affiliation:
Keywords: L-serine, Hydrazones, Cancer, Conagenin, Lymphokines, Antitumoral Evaluation, Streptomyces roseosporus, ceramidase inhibitors, apoptosis, tumor suppressor lipid, sphingosine kinase inhibitor, Pharmacological Studies, Melting points, IC50
Abstract: A series of 14 N-acyl-hydrazones L-serine derivatives have been synthesized and evaluated for their in vitro antitumoral activities against four neoplastic cancer cells: HL-60 (leukemia), MDA-MB-435 (melanoma), HCT-8 (colon) and SF-295 (nervous system). Five compounds (3g, 3h, 3i, 3k and 3n) were considered active against at least two cancer cell lines, with more than 90% of growth inhibition. Compound 3h, with IC50 of 2.04 μg/mL, seems to be moderately selective to HCT-8 and can be considered in further studies aiming new prototypes for a lead molecule against colon cancer.
Export Options
About this article
Cite this article as:
Carvalho Montenegro Raquel, Veras Costa Lotufo Leticia, Odorico de Moraes Manoel, do O Pessoa Claudia, Augusto Rocha Rodrigues Felipe, Campbell Pinheiro Alessandra, Cristina Mendonça Nogueira Thais and Vinicius Nora de Souza Marcus, Synthesis and Antitumoral Evaluation of Benzyl (1S)-2-[2-(monosubstituted-benzylidene)hydrazino]-1-(hydroxymethyl)-2-oxoethylcarbamate, Letters in Drug Design & Discovery 2012; 9 (3) . https://dx.doi.org/10.2174/157018012799129800
DOI https://dx.doi.org/10.2174/157018012799129800 |
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
-
Targeting Cellular Proapoptotic Molecules for Developing Anticancer Agents from Marine Sources
Current Drug Targets Modulation of Toll-Like Receptor 4. Insights from X-Ray Crystallography and Molecular Modeling
Current Topics in Medicinal Chemistry Function and Regulation of Let-7 Family microRNAs
MicroRNA NMR-based Metabolite Profiling of Pancreatic Cancer
Current Metabolomics Emerging Multi-cancer Regulatory Role of ESRP1: Orchestration of Alternative Splicing to Control EMT
Current Cancer Drug Targets Recent Advances in Small Molecule Inhibitors of VEGFR and EGFR Signaling Pathways
Current Topics in Medicinal Chemistry Local Treatment for Lymphoid Malignancies of the Eye
Anti-Cancer Agents in Medicinal Chemistry <i>In vivo</i> Evaluation of [<sup>225</sup>Ac]Ac-DOTA<sup>ZOL</sup> for α-Therapy of Bone Metastases
Current Radiopharmaceuticals A Role of DEAD-Box RNA Helicase rck/p54 in Cancer Cells
Current Drug Therapy Drug Delivery Systems for Prevention and Treatment of Osteoporotic Fracture
Current Drug Targets Review of Noscapine and its Analogues as Potential Anti-Cancer Drugs
Mini-Reviews in Organic Chemistry Aromatase, Estrogens and Testicular Germ Cell Development
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Central G-Protein Coupled Receptors (GPCR)s as Molecular Targets for the Treatment of Obesity: Assets, Liabilities and Development Status
Current Drug Targets - CNS & Neurological Disorders Fucose Specific Lectins in Cancer Research and Diagnosis
Drug Design Reviews - Online (Discontinued) MHC Class I TCR Engineered Anti-Tumor CD4 T Cells: Implications For Cancer Immunotherapy
Endocrine, Metabolic & Immune Disorders - Drug Targets Editorial (Thematic Issue: Signal Transduction of Natural Products for Anticancer Therapy)
Current Signal Transduction Therapy Baicalein - An Intriguing Therapeutic Phytochemical in Pancreatic Cancer
Current Drug Targets Lifestyle Factors and MicroRNAs: A New Paradigm in Cancer Chemoprevention
MicroRNA Protein Degradation Pathways after Brain Ischemia
Current Drug Targets Technetium Labeled Small Peptide Radiopharmaceuticals in the Identification of Lung Cancer
Current Pharmaceutical Design