Volume 18, Issue 24
Heterocyclic Compounds
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ChemInform Abstract: Anthrapyrazole Anticancer Agents. Synthesis and Structure-Activity Relationships Against Murine Leukemias.

H. D. H. SHOWALTER

H. D. H. SHOWALTER

Dep. Chem., Warner-Lambert/Parke-Davis Pharm. Res., Ann Arbor, MI 48105, USA

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J. L. JOHNSON

J. L. JOHNSON

Dep. Chem., Warner-Lambert/Parke-Davis Pharm. Res., Ann Arbor, MI 48105, USA

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J. M. HOFTIEZER

J. M. HOFTIEZER

Dep. Chem., Warner-Lambert/Parke-Davis Pharm. Res., Ann Arbor, MI 48105, USA

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W. R. TURNER

W. R. TURNER

Dep. Chem., Warner-Lambert/Parke-Davis Pharm. Res., Ann Arbor, MI 48105, USA

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L. M. WERBEL

L. M. WERBEL

Dep. Chem., Warner-Lambert/Parke-Davis Pharm. Res., Ann Arbor, MI 48105, USA

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W. R. LEOPOLD

W. R. LEOPOLD

Dep. Chem., Warner-Lambert/Parke-Davis Pharm. Res., Ann Arbor, MI 48105, USA

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J. L. SHILLIS

J. L. SHILLIS

Dep. Chem., Warner-Lambert/Parke-Davis Pharm. Res., Ann Arbor, MI 48105, USA

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R. C. JACKSON

R. C. JACKSON

Dep. Chem., Warner-Lambert/Parke-Davis Pharm. Res., Ann Arbor, MI 48105, USA

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E. F. ELSLAGER

E. F. ELSLAGER

Dep. Chem., Warner-Lambert/Parke-Davis Pharm. Res., Ann Arbor, MI 48105, USA

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First published: June 16, 1987

Abstract

The dichloroanthraquinones (I) and (VI) cyclize with the hydrazines (II) to give the chloroanthrapyrazoles (III) and (VII) respectively which are converted to the amino derivatives (V) and (IX) by reaction with the amines (IV) and (VIII).

ChemInform Abstract

The dichloroanthraquinones (I) and (VI) cyclize with the hydrazines (II) to give the chloroanthrapyrazoles (III) and (VII) respectively which are converted to the amino derivatives (V) and (IX) by reaction with the amines (IV) and (VIII). The antitumor activities of the compounds (V) and (IX) against L1210 leukemia in vitro and P388 leukemia in vivo are studied. (Comparison with doxorubicin and mitoxantrone, IR-, UV-, 1H-NMR-, pKa-data).

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