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Synthesis of imine-pyrazolopyrimidinones and their mechanistic interventions on anticancer activity |
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| Authors: | Ashish T. Baviskar Uttam C. Banerjee Mukesh Gupta Rajveer Singh Sunil Kumar Manish K. Gupta Sanjeev Kumar Satish K. Raut Madhu Khullar Sandeep Singh Raj Kumar |
| Affiliation: | 1. Laboratory for Drug Design and Synthesis, Centre for Chemical and Pharmaceutical Sciences, Central University of Punjab, 151 001 Bathinda, India;2. Department of Pharmaceutical Technology (Biotechnology), National Institute of Pharmaceutical Education and Research (NIPER), Mohali, S.A.S. Nagar, Sec 67, 160 062 Punjab, India;3. Molecular Modeling and Pharmacoinformatics Lab, Indo-Soviet Friendship College of Pharmacy, Moga, 141 001 Punjab, India;4. Centre for Biosciences, Central University of Punjab, 151 001 Bathinda, India;5. Centre for Genetic Diseases and Molecular Medicine, Central University of Punjab, 151 001 Bathinda, India;6. Department of Experimental Medicine and Biotechnology, PGIMER, 160 012 Chandigarh, India |
| Abstract: | Design, synthesis and anticancer activity of a series of imine-pyrazolopyrimidinones is reported for the first time. Compounds 9d, 9n and 9o in the series show encouraging in vitro anticancer activity with low micromolar IC50 values against prostate (PC3) and breast (MCF7) cancer cell lines. Some notions about structure–activity relationships and plausible mechanism of biological activity are presented. |
| Keywords: | Synthesis Imine-pyrazolopyrimidinones Anticancer agents Effects on G2/M phase of the cell cycle Catalytic topoisomerase inhibitors |
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