Cell Biological Manifestations of Bisdioxopiperazines: Treatment of Human Tumor Cell Lines in Culture

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Cell Biological Manifestations of Bisdioxopiperazines: Treatment of Human Tumor Cell Lines in Culture

Anti-Cancer Agents in Medicinal Chemistry, 10(9): 657-660.

Author(s): Da-Yong Lu, Ding-Ren Lu and Jian Ding.

Affiliation: School of Life Sciences, Shanghai University, Shanghai 200444, PR China.


British developed Bisdioxopiperazine compound (Biz compounds) {ICRF-159 or ICRF-187 (razoxane, Raz)} which was the first agent ever to be observed inhibiting and controlling the spontaneous pulmonary metastases of murine Lewis Lung Carcinoma (LLC) tumor model worldwide. Since 1980, two new Biz compounds {probimane (Pro, AT-2153, MST-2) and MST-16} have been synthesized at the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, PR China, based on structural modifications from British developed Biz compounds. Despite some similarities and differences of structural and pharmacological activities observed between Raz, Pro and MST-16, the systematic comparisons of their pharmacological activities and mechanisms, especially on neoplasm metastases, are still much needed. This work demonstrates that Biz compounds may inhibit tumor cell migration in vitro through a Matrigel-Coated Transwell plate assay and a wound-healing assay by using three human mammary tumor cell lines (MDA-MB-231, MDA-MB-435 and MDA-MB-468). Pro, ICRF-187 and MST-16 affect the network of actin assembly. We conclude that Biz compounds might inhibit neoplasm metastases via affecting a cascade of GTPases, cell skeleton polarizations and cell movements.


Bisdioxopiperazine compounds, razoxane, probimane, MST-16, neoplasm metastasis, cell movement, GTPses, actin, mammary cancer, MTX assay, cell migration.

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Article Details

Volume: 10
Issue Number: 9
First Page: 657
Last Page: 660
Page Count: 4
DOI: 10.2174/187152010794479843
Price: $58
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