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Synthesis and Biological Evaluation of Novel Acylhydrazone Derivatives as Potential Antitumor Agents

Synthesis and Biological Evaluation of Novel Acylhydrazone Derivatives as Potential Antitumor Agents

Cenzo Congiu, Valentina Onnis

Bioorg Med Chem. 2013 Nov 1;21(21):6592-9.

PMID: 24071449

Abstract:

We have designed, synthesized, and evaluated as potential antitumor agents a series of 2-hydroxybenzylidene derivatives of the N-(2-trifluoromethylpiridyn-4-yl)anthranilic acid hydrazide, and some analogues bearing a (2-trifluoromethyl)piridyn-4-ylamino group in 3- or 4-position of benzohydrazide or 4-position of phenylacetohydrazide. Compounds 12e, 13e, 15e, and 16e, bearing a 4-(diethylamino)salicylidene group exhibited potent cytotoxicity, with averaged GI50 values in sub-micromolar range, and a variety of cell selectivity at nanomolar concentrations. The determination of acute toxicity in athymic nudes mice proved some compounds to be non-toxic, making them good candidates for further study as antitumor agents.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP100139546	4-(Diethylamino)benzhydrazide		100139-54-6	Price

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