New anti-tumor agents.1. Heterocyclic benzodioxole lactones

Autor:	Leonard Jurd
Rok vydání:	1996
Předmět:	chemistry.chemical_classification Organic Chemistry Combinatorial chemistry In vitro chemistry.chemical_compound Acetic acid chemistry Acetylation Yield (chemistry) Organic chemistry Methanol Sesamol Tetronic acid Lactone
Zdroj:	Journal of Heterocyclic Chemistry. 33:1227-1232
ISSN:	1943-5193 0022-152X
DOI:	10.1002/jhet.5570330438
Popis:	Morpholino Mannich bases of types 5, 12 react with tetronic acid in aqueous acetic acid to yield uncyclized lactones of types 7, 13. Acetylation and methylation of these products yields monoacetyl-monomethyl derivatives which can then be cyclized in alkali to give unsaturated lactones of types 8, 16 and saturated lactones 9b, 15. The hydroxylactone 9a can be synthesized directly by reaction of 3,4,5-trimethoxybenzaldehyde with sesamol and tetronic acid in methanol. With few exceptions the lactones of type 8 and 16 have proven to be active inhibitors of tumor growth in the National Cancer Institute in vitro screening program against 60 diverse human cancer cell lines. The lactone 8 is particularly potent, inhibiting in vitro growth of some cancers at concentrations as low as 10−6-10−7 moles/1.
Databáze:	OpenAIRE
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