Potential Anticancer Agents: Design, Synthesis of New Pyrido[1,2-a]benzimidazoles and Related Derivatives Linked to Alkylating Fragments

@article{Darwish2018PotentialAA,
  title={Potential Anticancer Agents: Design, Synthesis of New Pyrido[1,2-a]benzimidazoles and Related Derivatives Linked to Alkylating Fragments},
  author={Salma Darwish and Rasha Y. Elbayaa and Hayam M. A. Ashour and Mounir A. Khalil and Elsayed Am Badawey},
  journal={Medicinal Chemistry},
  year={2018},
  volume={8},
  pages={1-10}
}
The incentive of the present work has been primarily directed towards the design and synthesis of some novel pyrido[1,2-a]benzimidazoles with specific functionalities believed to have alkylation ability. This combination of pharmacological agents may enable synergistic anticancer effect. Nine compounds 5b, 13a, 13d, 13e, 14b, 14c, 15, 16, and 17 were selected by the National Cancer Institute (NCI), Bethseda, Maryland, USA to be evaluated for their in vitro antitumor activity. All the selected… 
View via Publisher

Figures and Tables from this paper

References

SHOWING 1-10 OF 29 REFERENCES
Benzimidazole condensed ring systems. XII. Synthesis and anticancer evaluation of certain pyrido[1,2-a]benzimidazole derivatives.
TLDR
The synthesis and antineoplastic evaluation of related series of PBIs with similar haloarylamino, haloARYlamino-3-phenyl-PBI and haloarylazo moieties at position 1 or 2 reveal notable activity against some tumor cell lines.
Benzimidazole condensed ring systems 10 (1). Synthesis and cytotoxic activity of some pyrido[1,2-a]benzimidazoles.
TLDR
Compound (11, NSC 660334) exhibited a moderate in vitro antineoplastic activity especially against most of the leukemia cell lines, while compound (10, VM30309) showed a good cytotoxic activity against Artina salina larvae.
Benzimidazole condensed ring system. IX. Potential antineoplastics. New synthesis of some pyrido[1,2-α]benzimidazoles and related derivative
Benzimidazole condensed ring systems. XI. Synthesis of some substituted cycloalkyl pyrido[1,2-a]benzimidazoles with anticipated antineoplastic activity.
Facile synthesis of benzimidazole bearing 2-pyridone derivatives as potential antimicrobial agents
Diverse amide analogs of sulindac for cancer treatment and prevention.
The long and winding road for the development of tasquinimod as an oral second-generation quinoline-3-carboxamide antiangiogenic drug for the treatment of prostate cancer
  • J. Isaacs
  • Biology, Medicine
    Expert opinion on investigational drugs
  • 2010
TLDR
Tasquinimod is a novel inhibitor of tumor angiogenesis that enhances the therapeutic anticancer response when combined with other standard-of-care modalities in experimental animal models, but does not inhibit normal wound healing.
Some practical considerations and applications of the national cancer institute in vitro anticancer drug discovery screen
TLDR
Practical considerations and selected specific examples are selected, particularly illustrating research applications of the NCI screen that may be more broadly applicable to the search for new anticancer drug development leads with novel profiles of antitumor activity and/or mechanisms of action.
Feasibility of drug screening with panels of human tumor cell lines using a microculture tetrazolium assay.
TLDR
Since the microculture tetrazolium assay provides sensitive and reproducible indices of growth as well as drug sensitivity in individual cell lines over the course of multiple passages and several months' cultivation, it appears suitable for initial-stage in vitro drug screening.
Design, synthesis, and crystal structure of selective 2-pyridone tissue factor VIIa inhibitors.
TLDR
The pyridone core was selected as a replacement for the pyrazinone core of noncovalent tissue Factor VIIa inhibitors and designed such that their substitution pattern would occupy and interact with the S(1), S(2), and S(3) pockets of the tissuefactor VIIa enzyme.
...
...