Molecules, Vol. 24, Pages 2656: Structural and Biological Investigations for a Series of N-5 Substituted Pyrrolo3,2-dpyrimidines as Potential Anti-Cancer Therapeutics

Molecules, Vol. 24, Pages 2656: Structural and Biological Investigations for a Series of N-5 Substituted Pyrrolo[3,2-d]pyrimidines as Potential Anti-Cancer Therapeutics Molecules doi: 10.3390/molecules24142656 Authors: Brian M. Cawrse Nia’mani M. Robinson Nina C. Lee Gerald M. Wilson Katherine L. Seley-Radtke Pyrrolo[3,2-d]pyrimidines have been studied for many years as potential lead compounds for the development of antiproliferative agents. Much of the focus has been on modifications to the pyrimidine ring, with enzymatic recognition often modulated by C2 and C4 substituents. In contrast, this work focuses on the N5 of the pyrrole ring by means of a series of novel N5-substituted pyrrolo[3,2-d]pyrimidines. The compounds were screened against the NCI-60 Human Tumor Cell Line panel, and the results were analyzed using the COMPARE algorithm to elucidate potential mechanisms of action. COMPARE analysis returned strong correlation to known DNA alkylators and groove binders, corroborating the hypothesis that these pyrrolo[3,2-d]pyrimidines act as DNA or RNA alkylators. In addition, N5 substitution reduced the EC50 against CCRF-CEM leukemia cells by up to 7-fold, indicating that this position is of interest in the development of antiproliferative lead compounds based on the pyrrolo[3,2-d]pyrimidine scaffold.
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research

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Source: - Category: Research Source Type: clinical trials
(Natural News) The popularity of avocados has risen in recent years – not only because they are delicious, but because they are highly nutritious superfoods. One of the many health benefits they offer is their ability to ward off cancer. Avocados contain avocatin B, which is a compound found to fight against a type of...
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Source: Clinical Lymphoma Myeloma and Leukemia - Category: Cancer & Oncology Source Type: research
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Source: Anti-Cancer Drugs - Category: Cancer & Oncology Tags: Preclinical Papers Source Type: research
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Source: Journal of Experimental and Clinical Cancer Research - Category: Cancer & Oncology Authors: Tags: Correction Source Type: research
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