Synthesis of imine-pyrazolopyrimidinones and their mechanistic interventions on anticancer activity.
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.
Department of Pharmaceutical Technology, National Institute of Pharmaceutical Education and Research, Mohali, S.A.S. Nagar, Punjab, India.
Ashish T
AT
Baviskar
Uttam C
UC
Banerjee
Mukesh
M
Gupta
Rajveer
R
Singh
Sunil
S
Kumar
Manish K
MK
Gupta
Sanjeev
S
Kumar
Satish K
SK
Raut
Madhu
M
Khullar
Sandeep
S
Singh
Raj
R
Kumar
D000951:Antigens, Neoplasm / Q000737:chemistry / Q000378:metabolism; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D001665:Binding Sites; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004250:DNA Topoisomerases, Type II / Q000737:chemistry / Q000378:metabolism; D004268:DNA-Binding Proteins / Q000737:chemistry / Q000378:metabolism; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D059565:G2 Phase Cell Cycle Checkpoints / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D007097:Imines / Q000737:chemistry*; D059566:M Phase Cell Cycle Checkpoints / Q000187:drug effects; D061986:MCF-7 Cells; D062105:Molecular Docking Simulation; D017434:Protein Structure, Tertiary; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D013329:Structure-Activity Relationship
D000951:Antigens, Neoplasm; D000970:Antineoplastic Agents; D004268:DNA-Binding Proteins; D007097:Imines; D011720:Pyrazoles; D011725:Pyridines; C118531:pyrazolopyridine; D004250:DNA Topoisomerases, Type II
Anticancer agents; Catalytic topoisomerase inhibitors; Effects on G2/M phase of the cell cycle; Imine-pyrazolopyrimidinones; Synthesis