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

doi:10.3390/molecules24213922

Molecules (Oct 2019)

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

DOI: https://doi.org/10.3390/molecules24213922
Journal volume & issue: Vol. 24, no. 21
p. 3922

Abstract

Read online

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).

Published in Molecules

ISSN: 1420-3049 (Online)
Publisher: MDPI AG
Country of publisher: Switzerland
LCC subjects: Science: Chemistry: Organic chemistry
Website: http://www.mdpi.com/journal/molecules

About the journal

Abstract

Keywords