A lapachol derivative active against mouse lymphocytic leukemia P-388.

Abstract

Lapachol [2-hydroxy-3-(3-methyl-2-butenyl)-1,4-naphthoquinone] and its analogs [2-(3,7-dimethyl-2,6-octadienyl)-3-hydroxy-1,4-naphthoquinone and 2-(3,3-dibromo-2-propenyl)-3-hydroxy-1,4-naphthoquinone] have been described, among almost a hundred synthesized analogs, as active against rat tumor Walker 256 carcinosarcoma. The acetylglucosylation of lapachol results in a compound which extends lapachol activity becoming effective against mouse lymphocytic leukemia P-388. When mice inoculated with 10(6) leukemic cells were treated with the drug during 9 days, their life span increased 80% over the control animals. Identification spectral data (uv, ir, 1H NMR, and MS) of the compound obtained by synthesis are given.

• Authors: M da Consolação, F Linardi, M M de Oliveira, M R Sampaio
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 18 Issue 11 Pg. 1159-61 (Nov 1975) ISSN: 0022-2623 [Print] United States
• PMID: 1177264 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Naphthoquinones
• lapachol

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, therapeutic use)
• Carcinoma 256, Walker (drug therapy)
• Leukemia, Experimental (drug therapy)
• Mice
• Mice, Inbred C57BL
• Mice, Inbred DBA
• Naphthoquinones (chemical synthesis, therapeutic use)
• Rats