Preclinical Antitumor Activity and Pharmacokinetics of Methyl-2-Benzimidazolecarbamate (FB642)

@article{Hao2004PreclinicalAA,
  title={Preclinical Antitumor Activity and Pharmacokinetics of Methyl-2-Benzimidazolecarbamate (FB642)},
  author={Desir{\'e}e Hao and Jinee D. Rizzo and Stephanie Stringer and Rodney V. Moore and Jennifer Marty and Daniel L. Dexter and G L Mangold and James Berger Camden and Daniel D. Von Hoff and Steven D. Weitman},
  journal={Investigational New Drugs},
  year={2004},
  volume={20},
  pages={261-270}
}
Methyl-2-benzimidazolecarbamate(carbendazim, FB642) is an anticancer agentthat induces apoptosis of cancer cells. [] Key Result In the murineB16 melanoma model, T/C values > 200 wereobserved. In the human tumor xenograft,FB642 produced tumor growth inhibition ofgreater than 58% in five of the sevenxenograft models evaluated. Partial andcomplete tumor shrinkage was noted withFB642 against the MCF-7 breast tumor model.
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32 Citations
Background Citations
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32 Citations

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Preliminary investigation revealed that compounds 15 and 23 might bind with ct-DNA through the intercalation mode which is responsible for potent bioactivity, and transportation behaviour indicated that these molecules could efficiently bind to and be carried by bovine albumin, and the hydrogen bonding and hydrophobic interactions played important roles in interaction with serum albumin.
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Flow cytometric analysis revealed that these compounds arrest the cell cycle at G2/M phase and induced cell death by apoptosis and the apoptotic effects of compounds were confirmed by Hoechst staining, mitochondrial membrane potential, cytochrome c release, ROS generation, caspase 9 activation and DNA fragmentation analysis.
Original Research Paper SYNTHESIS, CYTOTOXIC EVALUATION AND MOLECULAR PROPERTIES STUDIES OF NOVEL BENZIMIDAZOLE DERIVATIVES WITH DITHIOCARBAMATE SIDE CHAIN
A series of new benzimidazole dithiocarbamates were synthesized and evaluated for antitumor activity against three cancer cell lines (A-549, MDA-MB and HT-29). The chemical structures of the…
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Abstract A series of new 2-[(5-substituted-1H-benzimidazol-2-yl)thio]-N-[4-[2-phenylthiazol-4-yl]phenyl]acetamide derivatives (4a–p) were synthesized according to the reported literature, and…
Effective synthesis of benzimidazoles-imidazo[1,2-a]pyrazine conjugates: A comparative study of mono-and bis-benzimidazoles for antitumor activity.
Synthesis, antiviral and antitumor activity of 2-substituted-5-amidino-benzimidazoles.
Design, synthesis and ADMET prediction of bis-benzimidazole as anticancer agent.
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