Synthesis of novel N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9-purine derivatives as inducers of apoptosis in MCF-7 breast cancer cells

• Published in: RSC advances 2016-02, Vol.6 (19), p.15286-15297
• Main Authors: Sunagar, Manjunath G, Gaonkar, Supreet, Sunagar, Santosh G, Deshapande, Narahari, Belavagi, Ningaraddi S, Khazi, Imtiyaz Ahmed M
• Format: Article
• ISSN: 2046-2069
• DOI: 10.1039/c5ra23242b

A series of N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9 H -purine derivatives ( PP05-PP21 ) were prepared and evaluated for their anticancer activity against a panel of human cancer cell lines. Evaluation of results revealed that some of the synthesized compounds exhibited promising anticancer activity against the examined cancer cell lines. The structure-activity relationship (SAR) studies in the present work revealed that simple N-9 alkyl substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9 H -purines are potent anticancer agents. Among all the compounds, PP17 (9- sec -butyl-6-(4-(4-propoxyphenyl)piperazin-1-yl)-9 H -purine) showed good inhibitory activity against MCF-7 cells. Cell cycle analysis of the compound suggested that induces G2/M phase arrest. Biochemical experiments showed that PP17 significantly induced MCF-7 cell apoptosis. Therefore, compound PP17 with a potent in vitro anticancer activity can serve as a promising lead compound for further study. A series of N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9 H -purine derivatives ( PP05-PP21 ) were prepared and evaluated for their anticancer activity against a panel of human cancer cell lines.