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新型噻吩取代的10-脱氮氨基蝶呤：合成与生物学评价。

New thiophene substituted 10-deazaaminopterins: synthesis and biological evaluation.

作者信息

Abraham A, McGuire J J, Galivan J, Vishnuvajjala B R, Nair M G

机构信息

University of South Alabama, Mobile 36688.

出版信息

Adv Exp Med Biol. 1993;338:421-4. doi: 10.1007/978-1-4615-2960-6_84.

DOI:10.1007/978-1-4615-2960-6_84
PMID:8304149
Abstract

Analogues of 10-deazaaminopterin (10-DAM) and 4-amino-4-deoxy-10-deazapteroyl-gamma-methylene glutamic acid (MDAM) in which the benzene ring was replaced with a thiophene ring have been synthesized and evaluated for their antitumor activity. These analogues were N-([5-(2,4-diamino-6-pteridinyl)ethyl]-2-thenoyl)-L- glutamic acid (1) and N-([5-(2,4-diamino-6-pteridinyl)ethyl]-2-thenoyl)-gamma-meth ylene glutamic acid (2).

摘要

已合成了苯环被噻吩环取代的10-脱氮氨基蝶呤（10-DAM）和4-氨基-4-脱氧-10-脱氮蝶酰-γ-亚甲基谷氨酸（MDAM）类似物，并对其抗肿瘤活性进行了评估。这些类似物为N-([5-(2,4-二氨基-6-蝶啶基)乙基]-2-噻吩甲酰基)-L-谷氨酸（1）和N-([5-(2,4-二氨基-6-蝶啶基)乙基]-2-噻吩甲酰基)-γ-亚甲基谷氨酸（2）。

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