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Mar. Drugs 2010, 8(7), 2129-2141; doi:10.3390/md8072129

Preclinical Pharmacology of BA-TPQ, a Novel Synthetic Iminoquinone Anticancer Agent

Division of Clinical Pharmacology, Department of Pharmacology and Toxicology, University of Alabama at Birmingham, Birmingham, AL 35294, USA
Department of Chemistry, University of Alabama at Birmingham, Birmingham, AL 35294, USA
Comprehensive Cancer Center, University of Alabama at Birmingham, Birmingham, Al 35294, USA
College of Preventive Medicine, The Third Military Medical University, Chongqing 400038, China
Author to whom correspondence should be addressed.
Received: 8 May 2010 / Revised: 11 June 2010 / Accepted: 8 July 2010 / Published: 13 July 2010
(This article belongs to the Special Issue Marine Drugs as Antitumour Agents)
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Marine natural products and their synthetic derivatives represent a major source of novel candidate anti-cancer compounds. We have recently tested the anti-cancer activity of more than forty novel compounds based on an iminoquinone makaluvamine scaffold, and have found that many of the compounds exert potent cytotoxic activity against human cancer cell lines. One of the most potent compounds, BA-TPQ [(11,12),7-(benzylamino)-1,3,4,8-tetrahydropyrrolo[4,3,2-de]quinolin-8(1H)-one], was active against a variety of human cancer cell lines, and inhibited the growth of breast and prostate xenograft tumors in mice. However, there was some toxicity noted in the mice following administration of the compound. In order to further the development of BA-TPQ, and in a search for potential sites of accumulation that might underlie the observed toxicity of the compound, we accomplished preclinical pharmacological studies of the compound. We herein report the in vitro and in vivo pharmacological properties of BA-TPQ, including its stability in plasma, plasma protein binding, metabolism by S9 enzymes, and plasma and tissue distribution. We believe these studies will be useful for further investigations, and may be useful for other investigators examining the use of similar compounds for cancer therapy. View Full-Text
Keywords: marine alkaloid; pharmacokinetics; protein binding; chemotherapy marine alkaloid; pharmacokinetics; protein binding; chemotherapy

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Ezell, S.J.; Li, H.; Xu, H.; Zhang, X.; Gurpinar, E.; Zhang, X.; Rayburn, E.R.; Sommers, C.I.; Yang, X.; Velu, S.E.; Wang, W.; Zhang, R. Preclinical Pharmacology of BA-TPQ, a Novel Synthetic Iminoquinone Anticancer Agent. Mar. Drugs 2010, 8, 2129-2141.

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