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N7-Substituted 7-aminoactinomycin D Analogues. Synthesis and Biological Properties

N7-Substituted 7-aminoactinomycin D Analogues. Synthesis and Biological Properties

M S Madhavarao, M Chaykovsky, S K Sengupta

J Med Chem. 1978 Sep;21(9):958-61.

PMID: 722760

Abstract:

A series of N7-substituted 7-aminoactinomycin D analogues with alkyl, aralkyl, and heteroaralkyl substituents was synthesized and their biological properties were studied. All of these analogues proved to be 22- to 28-fold less toxic than actinomycin D when tested against human lymphoblastic leukemia cells (CCRF-CEM) in vitro. Against the P388 mouse leukemia in vivo, most of the analogues had activity comparable to actinomycin D and one was significantly more active. The results show that substitutions of this kind do not interfere with the antitumor activity of actinomycin D and may be useful for the design of modified actinomycin D analogues with greater selectivity.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP7240371-A	7-Aminoactinomycin D		7240-37-1	Price

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