Potential antitumor agents. 50. In vivo solid-tumor activity of derivatives of N-[2-(dimethylamino)ethyl]acridine-4-carboxamide.

doi:10.1021/JM00387A014

Paper

Potential antitumor agents. 50. In vivo solid-tumor activity of derivatives of N-[2-(dimethylamino)ethyl]acridine-4-carboxamide.

Published Apr 1, 1987 · G. Atwell, G. Rewcastle, B. Baguley

Journal of medicinal chemistry

Q1 SJR score

179

Citations

2

Influential Citations

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Abstract

The synthesis, physicochemical properties, and antitumor activity of a series of N-[2-(dialkylamino)alkyl]-acridine-4-carboxamides are reported. The compounds bind to DNA by intercalation, but exist under physiological conditions as monocations due to the weakly basic acridine chromophore (pKa = 3.5-4.5). The acridine-4-carboxamides show very broad structure-activity relationships (SAR) for antileukemic activity, with substituents at nearly all acridine positions proving acceptable. The compounds also show remarkable activity against the Lewis lung solid tumor in vivo, with several analogues capable of effecting 100% cures of the advanced disease. The broad SAR and high solid-tumor activity of the 9-acridine-4-carboxamides imply they should be considered as a completely new class of antitumor agent.

In Vitro Study

Highly Cited

Study Snapshot

N-[2-(dialkylamino)alkyl]-acridine-4-carboxamides show broad antileukemic activity and high solid-tumor activity, suggesting they could be a new class of antitumor agents.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Potential antitumor agents. 50. In vivo solid-tumor activity of derivatives of N-[2-(dimethylamino)ethyl]acridine-4-carboxamide.

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References

Citations

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Design, Synthesis and Evaluation of Photophysical and Biological Properties of Tetrafluoroacridine

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Recent Advances in the Synthesis of Fused‐Cyclic Quinolines

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Palladium-Catalyzed Chelation-Assisted Aldehyde C-H Bond Activation of Quinoline-8-carbaldehydes: Synthesis of Amides from Aldehydes with Anilines and Other Amines.

Palladium-catalyzed chelation-assisted direct aldehyde C-H bond amidation of quinoline-8-carbaldehydes with an amine effectively synthesizes amides, which can be applied to DNA intercalating agents.

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This study presents a simple method for synthesis of indeno-[1,2-b]-quinoline-9,11-(6H,10H)-dione derivatives and 7,7-dimethyl-10-aryl-7,8-dihydro-5H-indeno[1,2-b]

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Novel DNA Bis-Intercalator XR5944 as a Potent Anticancer Drug—Design and Mechanism of Action

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