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


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).

SUBMITTER: Yadav Y 

PROVIDER: S-EPMC6864788 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature

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

Yadav Yogesh Y   Sharma Deepti D   Kaushik Kumar K   Kumar Vineet V   Jha Amitabh A   Prasad Ashok K AK   Len Christophe C   Malhotra Sanjay V SV   Wengel Jesper J   Parmar Virinder S VS  

Molecules (Basel, Switzerland) 20191030 21


The synthesis of novel pyrazolylnucleosides <b>3a</b>-<b>e</b>, <b>4a</b>-<b>e</b>, <b>5a</b>-<b>e</b>, and <b>6a</b>-<b>e</b> are described. The structures of the regioisomers were elucidated by using extensive NMR studies. The pyrazolylnucleosides <b>5a</b>-<b>e</b> and <b>6a</b>-<b>e</b> were screened for anticancer activities on sixty human tumor cell lines. The compound <b>6e</b> showed good activity against 39 cancer cell lines. In particular, it showed significant inhibition against the l  ...[more]

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