Syntheses, Molecular Targets and Antitumor Activities of Novel Triptycene Bisquinones and 1,4-Anthracenedione Analogs

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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  • 27th of 59 in Chemistry, Medicinal

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

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Syntheses, Molecular Targets and Antitumor Activities of Novel Triptycene Bisquinones and 1,4-Anthracenedione Analogs

Anti-Cancer Agents in Medicinal Chemistry, 6(4): 303-318.

Author(s): Duy H. Hua, Kaiyan Lou, Srinivas K. Battina, Huiping Zhao, Elisabeth M Perchellet, Yang Wang and Jean-Pierre H Perchellet.

Affiliation: Department of Chemistry Kansas State University, 111 Willard Hall, Manhattan, KS 66506-3701,USA.


Novel substituted triptycene bisquinones and 1, 4-anthracenediones were synthesized and screened for their anti-cancer activities. A number of analogs were synthesized utilizing various synthetic transformations and found to elicit interesting antitumor effects. Analogs included water-soluble pro-drugs and ammonium salts. These potent antitumor drugs are DNA topoisomerase inhibitors that induce DNA strand breaks, inhibit DNA, RNA and protein syntheses and reduce tumor cell proliferation in the nanomolar range in vitro. They induce cytochrome c release, caspase-9, -3 and -8 activities, poly(ADP)-ribose polymerase-1 (PARP) cleavage, and internucleosomal DNA fragmentation by a mechanism which involves caspase-2 activation but not Fas signaling. Moreover, these drugs remain effective in multidrug-resistant tumor cells and have the advantage of blocking nucleoside transport and inducing a rapid loss of mitochondrial transmembrane potential. Based on their effects in tumor cells and isolated mitochondria, it is hypothesized that these drugs might, directly and indirectly, target components of the permeability transition pore to induce mitochondrial permeability transition and the release of proapoptotic factors. This review provides a summary of synthetic efforts and mechanistic endeavor.


Triptycene bisquinones, 4-anthracenediones, antitumor agents, mitochondrial permeability transition, DNA topoisomerase inhibitors, caspase activities, poly(ADP-ribose) polymerase-1 cleavage, pro-drugs.

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Article Details

Volume: 6
Issue Number: 4
First Page: 303
Last Page: 318
Page Count: 16
DOI: 10.2174/187152006777698141
Price: $58
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