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.
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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 |
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