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

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

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Abstract

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).

Original languageEnglish
Article number3922
JournalMolecules
Volume24
Issue number21
Number of pages16
ISSN1420-3049
DOIs
Publication statusPublished - 30. Oct 2019

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cultured cells
Cells
Cell Line
evaluation
cancer
Humulus
Tumor Cell Line
breast
lungs
Tumors
tumors
Nuclear magnetic resonance
nuclear magnetic resonance
Neoplasms
synthesis

Keywords

  • Anticancer
  • Modified nucleosides
  • NCI-60
  • NOESY study
  • Pyrazolylnucleosides

Cite this

Yadav, Y., Sharma, D., Kaushik, K., Kumar, V., Jha, A., Prasad, A. K., ... Parmar, V. S. (2019). Synthetic, structural, and anticancer activity evaluation studies on novel pyrazolylnucleosides. Molecules, 24(21), [3922]. https://doi.org/10.3390/molecules24213922
Yadav, Yogesh ; Sharma, Deepti ; Kaushik, Kumar ; Kumar, Vineet ; Jha, Amitabh ; Prasad, Ashok K. ; Len, Christophe ; Malhotra, Sanjay V. ; Wengel, Jesper ; Parmar, Virinder S. / Synthetic, structural, and anticancer activity evaluation studies on novel pyrazolylnucleosides. In: Molecules. 2019 ; Vol. 24, No. 21.
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abstract = "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).",
keywords = "Anticancer, Modified nucleosides, NCI-60, NOESY study, Pyrazolylnucleosides",
author = "Yogesh Yadav and Deepti Sharma and Kumar Kaushik and Vineet Kumar and Amitabh Jha and Prasad, {Ashok K.} and Christophe Len and Malhotra, {Sanjay V.} and Jesper Wengel and Parmar, {Virinder S.}",
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Yadav, Y, Sharma, D, Kaushik, K, Kumar, V, Jha, A, Prasad, AK, Len, C, Malhotra, SV, Wengel, J & Parmar, VS 2019, 'Synthetic, structural, and anticancer activity evaluation studies on novel pyrazolylnucleosides', Molecules, vol. 24, no. 21, 3922. https://doi.org/10.3390/molecules24213922

Synthetic, structural, and anticancer activity evaluation studies on novel pyrazolylnucleosides. / Yadav, Yogesh; Sharma, Deepti; Kaushik, Kumar; Kumar, Vineet; Jha, Amitabh; Prasad, Ashok K.; Len, Christophe; Malhotra, Sanjay V.; Wengel, Jesper; Parmar, Virinder S.

In: Molecules, Vol. 24, No. 21, 3922, 30.10.2019.

Research output: Contribution to journalJournal articleResearchpeer-review

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T1 - Synthetic, structural, and anticancer activity evaluation studies on novel pyrazolylnucleosides

AU - Yadav, Yogesh

AU - Sharma, Deepti

AU - Kaushik, Kumar

AU - Kumar, Vineet

AU - Jha, Amitabh

AU - Prasad, Ashok K.

AU - Len, Christophe

AU - Malhotra, Sanjay V.

AU - Wengel, Jesper

AU - Parmar, Virinder S.

PY - 2019/10/30

Y1 - 2019/10/30

N2 - 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).

AB - 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).

KW - Anticancer

KW - Modified nucleosides

KW - NCI-60

KW - NOESY study

KW - Pyrazolylnucleosides

U2 - 10.3390/molecules24213922

DO - 10.3390/molecules24213922

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JF - Molecules

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