Anti-Cancer Agents in Medicinal Chemistry

(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Michelle Prudhomme  
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France

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Different 6-Aryl-Fulvenes Exert Anti-proliferative effects on Cancer Cells

Author(s): Esther Sirignano, Assunta Pisano, Anna Caruso, Carmela Saturnino, Maria Stefania Sinicropi, Rosamaria Lappano, Antonio Botta, Domenico Iacopetta, Marcello Maggiolini, Pasquale Longo.

Graphical Abstract:


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.

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Article Details

VOLUME: 15
ISSUE: 4
Page: [468 - 474]
Pages: 7
DOI: 10.2174/1871520614666141019190855
Price: $58