Cargando…

Synthetic, Structural, and Anticancer Activity Evaluation Studies on Novel Pyrazolylnucleosides

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 sho...

Descripción completa

Detalles Bibliográficos
Autores principales: Yadav, Yogesh, Sharma, Deepti, Kaushik, Kumar, Kumar, Vineet, Jha, Amitabh, Prasad, Ashok K., Len, Christophe, Malhotra, Sanjay V., Wengel, Jesper, Parmar, Virinder S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6864788/
https://www.ncbi.nlm.nih.gov/pubmed/31671703
http://dx.doi.org/10.3390/molecules24213922
_version_ 1783471961323601920
author Yadav, Yogesh
Sharma, Deepti
Kaushik, Kumar
Kumar, Vineet
Jha, Amitabh
Prasad, Ashok K.
Len, Christophe
Malhotra, Sanjay V.
Wengel, Jesper
Parmar, Virinder S.
author_facet Yadav, Yogesh
Sharma, Deepti
Kaushik, Kumar
Kumar, Vineet
Jha, Amitabh
Prasad, Ashok K.
Len, Christophe
Malhotra, Sanjay V.
Wengel, Jesper
Parmar, Virinder S.
author_sort Yadav, Yogesh
collection PubMed
description 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 (GI(50) 9.3 µM) and breast cancer cell line HS 578T (GI(50) 3.0 µM).
format Online
Article
Text
id pubmed-6864788
institution National Center for Biotechnology Information
language English
publishDate 2019
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-68647882019-12-06 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. Molecules Article 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 (GI(50) 9.3 µM) and breast cancer cell line HS 578T (GI(50) 3.0 µM). MDPI 2019-10-30 /pmc/articles/PMC6864788/ /pubmed/31671703 http://dx.doi.org/10.3390/molecules24213922 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
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
title Synthetic, Structural, and Anticancer Activity Evaluation Studies on Novel Pyrazolylnucleosides
title_full Synthetic, Structural, and Anticancer Activity Evaluation Studies on Novel Pyrazolylnucleosides
title_fullStr Synthetic, Structural, and Anticancer Activity Evaluation Studies on Novel Pyrazolylnucleosides
title_full_unstemmed Synthetic, Structural, and Anticancer Activity Evaluation Studies on Novel Pyrazolylnucleosides
title_short Synthetic, Structural, and Anticancer Activity Evaluation Studies on Novel Pyrazolylnucleosides
title_sort synthetic, structural, and anticancer activity evaluation studies on novel pyrazolylnucleosides
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6864788/
https://www.ncbi.nlm.nih.gov/pubmed/31671703
http://dx.doi.org/10.3390/molecules24213922
work_keys_str_mv AT yadavyogesh syntheticstructuralandanticanceractivityevaluationstudiesonnovelpyrazolylnucleosides
AT sharmadeepti syntheticstructuralandanticanceractivityevaluationstudiesonnovelpyrazolylnucleosides
AT kaushikkumar syntheticstructuralandanticanceractivityevaluationstudiesonnovelpyrazolylnucleosides
AT kumarvineet syntheticstructuralandanticanceractivityevaluationstudiesonnovelpyrazolylnucleosides
AT jhaamitabh syntheticstructuralandanticanceractivityevaluationstudiesonnovelpyrazolylnucleosides
AT prasadashokk syntheticstructuralandanticanceractivityevaluationstudiesonnovelpyrazolylnucleosides
AT lenchristophe syntheticstructuralandanticanceractivityevaluationstudiesonnovelpyrazolylnucleosides
AT malhotrasanjayv syntheticstructuralandanticanceractivityevaluationstudiesonnovelpyrazolylnucleosides
AT wengeljesper syntheticstructuralandanticanceractivityevaluationstudiesonnovelpyrazolylnucleosides
AT parmarvirinders syntheticstructuralandanticanceractivityevaluationstudiesonnovelpyrazolylnucleosides