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多种α-萘胺衍生物的细胞毒性和抗真菌活性

Cytotoxic and Antifungal Activities of Diverse α-Naphthylamine Derivatives.

作者信息

Kouznetsov Vladímir V, Zacchino Susana A, Sortino Maximiliano, Vargas Méndez Leonor Y, Gupta Mahabir P

机构信息

Laboratorio de Química Orgánica y Biomolecular, Escuela de Química, Universidad Industrial de Santander, A. A. 678, Bucaramanga, Colombia.

出版信息

Sci Pharm. 2012 Oct-Dec;80(4):867-77. doi: 10.3797/scipharm.1209-03. Epub 2012 Oct 23.

Abstract

Diverse α-naphthylamine derivatives were easily prepared from corresponding aldimines derived from commercially available α-naphthaldehyde and anilines or isomeric pyridinecarboxyaldehydes and α-naphthylamine. The secondary amines obtained were tested as possible antifungal and cytotoxic agents. The diverse N-aryl-N-[1-(1-naphthyl)but-3-enyl]amines obtained were active (IC(50) < 10 μg/mL) against breast (MCF-7), non-small cell lung (H-460), and central nervous system (SF-268) human cancer cell lines, while N-(pyridinylmethyl)-naphthalen-1-amines resulted in activity against (MIC 25-32 μg/mL) some human opportunistic pathogenic fungi including yeasts, hialohyphomycetes, and dermatophytes.

摘要

多种α-萘胺衍生物可轻松由市售α-萘甲醛与苯胺或异构吡啶甲醛及α-萘胺衍生的相应醛亚胺制备而成。所得到的仲胺作为可能的抗真菌和细胞毒性剂进行了测试。所得到的多种N-芳基-N-[1-(1-萘基)丁-3-烯基]胺对人乳腺癌(MCF-7)、非小细胞肺癌(H-460)和中枢神经系统(SF-268)癌细胞系具有活性(IC(50) < 10 μg/mL),而N-(吡啶基甲基)-萘-1-胺对包括酵母、透明丝孢霉和皮肤癣菌在内的一些人类机会致病真菌具有活性(MIC 25 - 32 μg/mL)。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5ee5/3528049/904fcf7e345f/scipharm-2012-80-867f1.jpg

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