Abstract
Fulvenes represent a class of molecules very interesting under a chemical point of view because are easily accessible starting materials and are still poorly characterized for their biological activities, with the exception of acylfulvene and irofulvenes which have been reported to exert cytotoxic properties. Here, we describe the synthesis and characterization of several aryl-fulvenes together with their effects on cancer cell growth by MTT method. The cytotoxic potential was investigated on a panel of tumor cell lines such as breast MCF7 and SkBr3, endometrial Ishikawa, prostate LnCaP and lung A549, in comparison with the cis-diamminedichloroplatinum(II) (cisplatin) which is largely used for the treatment of different types of cancer. The evaluation of the cytotoxic activity of these compounds indicated that they are able to inhibit the proliferation of the aforementioned cancer cell types. In particular, the compound 4 exhibited the most powerful antiproliferative activity on all tumor cells evaluated with higher inhibitory effects respect to cisplatin and without altering the proliferation of human mammary MCF-10A epithelial cells.
Keywords: Antiproliferative activity, A549, Fulvenes, Ishikawa, LnCaP, MCF-10A, MCF7, SkBr3.
Anti-Cancer Agents in Medicinal Chemistry
Title:Different 6-Aryl-Fulvenes Exert Anti-proliferative effects on Cancer Cells
Volume: 15 Issue: 4
Author(s): Esther Sirignano, Assunta Pisano, Anna Caruso, Carmela Saturnino, Maria Stefania Sinicropi, Rosamaria Lappano, Antonio Botta, Domenico Iacopetta, Marcello Maggiolini and Pasquale Longo
Affiliation:
Keywords: Antiproliferative activity, A549, Fulvenes, Ishikawa, LnCaP, MCF-10A, MCF7, SkBr3.
Abstract: Fulvenes represent a class of molecules very interesting under a chemical point of view because are easily accessible starting materials and are still poorly characterized for their biological activities, with the exception of acylfulvene and irofulvenes which have been reported to exert cytotoxic properties. Here, we describe the synthesis and characterization of several aryl-fulvenes together with their effects on cancer cell growth by MTT method. The cytotoxic potential was investigated on a panel of tumor cell lines such as breast MCF7 and SkBr3, endometrial Ishikawa, prostate LnCaP and lung A549, in comparison with the cis-diamminedichloroplatinum(II) (cisplatin) which is largely used for the treatment of different types of cancer. The evaluation of the cytotoxic activity of these compounds indicated that they are able to inhibit the proliferation of the aforementioned cancer cell types. In particular, the compound 4 exhibited the most powerful antiproliferative activity on all tumor cells evaluated with higher inhibitory effects respect to cisplatin and without altering the proliferation of human mammary MCF-10A epithelial cells.
Export Options
About this article
Cite this article as:
Sirignano Esther, Pisano Assunta, Caruso Anna, Saturnino Carmela, Sinicropi Stefania Maria, Lappano Rosamaria, Botta Antonio, Iacopetta Domenico, Maggiolini Marcello and Longo Pasquale, Different 6-Aryl-Fulvenes Exert Anti-proliferative effects on Cancer Cells, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (4) . https://dx.doi.org/10.2174/1871520614666141019190855
DOI https://dx.doi.org/10.2174/1871520614666141019190855 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- 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
-
Synthesis of bis(indolyl)methanes Using Naturally Occurring, Biodegradable Itaconic Acid as a Green and Reusable Catalyst
Current Organic Synthesis The Antiprogestogen Mifepristone: A Review
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Clinical Applicability of Microarray Technology in the Diagnosis, Prognostic Stratification, Treatment and Clinical Surveillance of Cervical Adenocarcinoma
Current Pharmaceutical Design Applied Proteomics in Companion Animal Medicine
Current Proteomics Role of C1QBP/p32 and its Therapeutic Potential in Breast Carcinoma and other Cancers
Current Medicinal Chemistry Emerging Multi-cancer Regulatory Role of ESRP1: Orchestration of Alternative Splicing to Control EMT
Current Cancer Drug Targets The Potential Clinical Impact of Probiotic Treatment for the Prevention and/or Anti-Inflammatory Therapeutic Effect Against Radiation Induced Intestinal Mucositis. A Review
Recent Patents on Inflammation & Allergy Drug Discovery Photomedical Approaches for the Diagnosis and Treatment of Gynecologic Cancers
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Advancements in Treatment Options of Women Infertility
Current Women`s Health Reviews LHRH-Targeted Drug Delivery Systems for Cancer Therapy
Mini-Reviews in Medicinal Chemistry Developing Phytoestrogens for Breast Cancer Prevention
Anti-Cancer Agents in Medicinal Chemistry Personalizing HER2-Targeted Therapy in Metastatic Breast Cancer Beyond HER2 Status: What We Have Learned from Clinical Specimens
Current Pharmacogenomics and Personalized Medicine Immunological Puzzle Related to Recurrent Miscarriage: Overview
Current Immunology Reviews (Discontinued) Trabectedin (Yondelis®) as a Therapeutic Option in Gynecological Cancers: A Focus on its Mechanisms of Action, Clinical Activity and Genomic Predictors of Drug Response
Current Drug Targets New Peptidic GnRH Antagonists Offer a Broad Range of Therapeutic Applications
Letters in Drug Design & Discovery SPECT-CT and PET-CT in Oncology - An Overview
Current Medical Imaging Aldose Reductase Enzyme and its Implication to Major Health Problems of the 21st Century
Current Medicinal Chemistry Estrogen Regulation of MicroRNA Expression
Current Genomics Clomiphene Citrate, Metformin or Both for Ovulation Induction in Therapy Naïve Women with Polycystic Ovary Syndrome (PCOS)? A Descriptive Review
Current Drug Therapy Possible Role of PTEN Expression in Discriminating Benign Endometrial Hyperplasia from Atypical Hyperplasia/Endometrial Intraepithelial Neoplasia in a Series of Egyptian Patients
Current Women`s Health Reviews