Synthetic, Structural, and Anticancer Activity Evaluation Studies on Novel Pyrazolylnucleosides
Yogesh Yadav,
Deepti Sharma,
Kumar Kaushik,
Vineet Kumar,
Amitabh Jha,
Ashok K. Prasad,
Christophe Len,
Sanjay V. Malhotra,
Jesper Wengel,
Virinder S. Parmar
Affiliations
Yogesh Yadav
Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India
Deepti Sharma
Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India
Kumar Kaushik
Department of Chemistry and Environmental Science, Medgar Evers College, The City University of New York, 1638 Bedford Avenue, Brooklyn, NY 11225, USA
Vineet Kumar
Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India
Amitabh Jha
Medicinal Chemistry Laboratory, Department of Chemistry, Acadia University, Wolfville, NS B4P 2R6, Canada
Ashok K. Prasad
Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India
Christophe Len
Chimie ParisTech, PSL University, CNRS Institute of Chemistry for Life and Health Sciences—i-CLeHS, 11 rue Pierre et Marie Curie, F-75005 Paris, France
Sanjay V. Malhotra
Laboratory of Synthetic Chemistry, Leidos Biomedical Research Inc., Frederick National Laboratory for Cancer Research, Frederick, MD 2170, USA
Jesper Wengel
Nucleic Acid Center, Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, DK-5230 Odense, Denmark
Virinder S. Parmar
Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India
The synthesis of novel pyrazolylnucleosides 3a−e, 4a−e, 5a−e, and 6a−e are described. The structures of the regioisomers were elucidated by using extensive NMR studies. The pyrazolylnucleosides 5a−e and 6a−e were screened for anticancer activities on sixty human tumor cell lines. The compound 6e showed good activity against 39 cancer cell lines. In particular, it showed significant inhibition against the lung cancer cell line Hop-92 (GI50 9.3 µM) and breast cancer cell line HS 578T (GI50 3.0 µM).
