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

Autor:	Ningaraddi S. Belavagi, Manjunath G. Sunagar, Narahari Deshapande, Imtiyaz Ahmed M. Khazi, Supreet Gaonkar, Santosh G. Sunagar
Rok vydání:	2016
Předmět:	010405 organic chemistry Chemistry Stereochemistry General Chemical Engineering General Chemistry 010402 general chemistry 01 natural sciences In vitro 0104 chemical sciences chemistry.chemical_compound MCF-7 Cell culture Apoptosis Purine derivative Inducer Breast cancer cells Lead compound
Zdroj:	RSC Advances. 6:15286-15297
ISSN:	2046-2069
Popis:	A series of N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-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)-9H-purines are potent anticancer agents. Among all the compounds, PP17 (9-sec-butyl-6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::9a59f65a73e8cdf07e379333d9e4ef67 https://doi.org/10.1039/c5ra23242b Zobrazit plný text záznamu