Synthetic, Structural, and Anticancer Activity Evaluation Studies on Novel Pyrazolylnucleosides
Identifieur interne : 000D17 ( Main/Merge ); précédent : 000D16; suivant : 000D18Synthetic, Structural, and Anticancer Activity Evaluation Studies on Novel Pyrazolylnucleosides
Auteurs : Yogesh Yadav [Inde] ; Deepti Sharma [Inde] ; Kumar Kaushik ; Vineet Kumar [États-Unis] ; Amitabh Jha ; Ashok K. Prasad ; Christophe Len [France] ; Sanjay V. Malhotra [États-Unis] ; Jesper Wengel ; Virinder S. ParmarSource :
- Molecules [ 1420-3049 ] ; 2019.
Abstract
The synthesis of novel pyrazolylnucleosides
Url:
DOI: 10.3390/molecules24213922
PubMed: 31671703
PubMed Central: 6864788
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PMC:6864788Le document en format XML
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(Y.Y.);<email>iamvineet@gmail.com</email>
(V.K.);<email>ashokenzyme@gmail.com</email>
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<affiliation><nlm:aff id="af2-molecules-24-03922">Medicinal Chemistry Laboratory, Department of Chemistry, Acadia University, Wolfville, NS B4P 2R6, Canada;<email>amitabh.jha@acadiau.ca</email>
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<author><name sortKey="Len, Christophe" sort="Len, Christophe" uniqKey="Len C" first="Christophe" last="Len">Christophe Len</name>
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</nlm:aff>
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<author><name sortKey="Parmar, Virinder S" sort="Parmar, Virinder S" uniqKey="Parmar V" first="Virinder S." last="Parmar">Virinder S. Parmar</name>
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(Y.Y.);<email>iamvineet@gmail.com</email>
(V.K.);<email>ashokenzyme@gmail.com</email>
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<affiliation><nlm:aff id="af5-molecules-24-03922">Department of Chemistry and Environmental Science, Medgar Evers College, The City University of New York, 1638 Bedford Avenue, Brooklyn, NY 11225, USA;<email>kumar.kaushik.drdo@gmail.com</email>
</nlm:aff>
</affiliation>
<affiliation><nlm:aff id="af9-molecules-24-03922">Nucleic Acid Center, Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, DK-5230 Odense, Denmark;<email>jwe@sdu.dk</email>
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<sourceDesc><biblStruct><analytic><title xml:lang="en" level="a" type="main">Synthetic, Structural, and Anticancer Activity Evaluation Studies on Novel Pyrazolylnucleosides</title>
<author><name sortKey="Yadav, Yogesh" sort="Yadav, Yogesh" uniqKey="Yadav Y" first="Yogesh" last="Yadav">Yogesh Yadav</name>
<affiliation><nlm:aff id="af1-molecules-24-03922">Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India;<email>yogeshyadav77@gmail.com</email>
(Y.Y.);<email>iamvineet@gmail.com</email>
(V.K.);<email>ashokenzyme@gmail.com</email>
(A.K.P.)</nlm:aff>
</affiliation>
<affiliation><nlm:aff id="af2-molecules-24-03922">Medicinal Chemistry Laboratory, Department of Chemistry, Acadia University, Wolfville, NS B4P 2R6, Canada;<email>amitabh.jha@acadiau.ca</email>
</nlm:aff>
</affiliation>
<affiliation wicri:level="1"><nlm:aff id="af3-molecules-24-03922">SUN Pharmaceuticals R&D, Gurgaon, Sarhaul, Sector-18, Haryana-122 015, India</nlm:aff>
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<author><name sortKey="Sharma, Deepti" sort="Sharma, Deepti" uniqKey="Sharma D" first="Deepti" last="Sharma">Deepti Sharma</name>
<affiliation><nlm:aff id="af1-molecules-24-03922">Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India;<email>yogeshyadav77@gmail.com</email>
(Y.Y.);<email>iamvineet@gmail.com</email>
(V.K.);<email>ashokenzyme@gmail.com</email>
(A.K.P.)</nlm:aff>
</affiliation>
<affiliation wicri:level="1"><nlm:aff id="af4-molecules-24-03922">Sri Venkateswara College, Benito Juarez Road, Dhaula Kuan, University of Delhi, Delhi 110 021, India</nlm:aff>
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<author><name sortKey="Kaushik, Kumar" sort="Kaushik, Kumar" uniqKey="Kaushik K" first="Kumar" last="Kaushik">Kumar Kaushik</name>
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</nlm:aff>
</affiliation>
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<author><name sortKey="Kumar, Vineet" sort="Kumar, Vineet" uniqKey="Kumar V" first="Vineet" last="Kumar">Vineet Kumar</name>
<affiliation><nlm:aff id="af1-molecules-24-03922">Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India;<email>yogeshyadav77@gmail.com</email>
(Y.Y.);<email>iamvineet@gmail.com</email>
(V.K.);<email>ashokenzyme@gmail.com</email>
(A.K.P.)</nlm:aff>
</affiliation>
<affiliation><nlm:aff id="af6-molecules-24-03922">Laboratory of Synthetic Chemistry, Leidos Biomedical Research Inc., Frederick National Laboratory for Cancer Research, Frederick, MD 2170, USA;<email>smalhotra@stanford.edu</email>
</nlm:aff>
</affiliation>
<affiliation wicri:level="2"><nlm:aff id="af7-molecules-24-03922">Department of Radiation Oncology, Stanford University, 1050A Arastradero Road, A252, Palo Alto, CA 94304, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Radiation Oncology, Stanford University, 1050A Arastradero Road, A252, Palo Alto, CA 94304</wicri:regionArea>
<placeName><region type="state">Californie</region>
</placeName>
</affiliation>
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<author><name sortKey="Jha, Amitabh" sort="Jha, Amitabh" uniqKey="Jha A" first="Amitabh" last="Jha">Amitabh Jha</name>
<affiliation><nlm:aff id="af2-molecules-24-03922">Medicinal Chemistry Laboratory, Department of Chemistry, Acadia University, Wolfville, NS B4P 2R6, Canada;<email>amitabh.jha@acadiau.ca</email>
</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Prasad, Ashok K" sort="Prasad, Ashok K" uniqKey="Prasad A" first="Ashok K." last="Prasad">Ashok K. Prasad</name>
<affiliation><nlm:aff id="af1-molecules-24-03922">Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India;<email>yogeshyadav77@gmail.com</email>
(Y.Y.);<email>iamvineet@gmail.com</email>
(V.K.);<email>ashokenzyme@gmail.com</email>
(A.K.P.)</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Len, Christophe" sort="Len, Christophe" uniqKey="Len C" first="Christophe" last="Len">Christophe Len</name>
<affiliation wicri:level="3"><nlm:aff id="af8-molecules-24-03922">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</nlm:aff>
<country xml:lang="fr">France</country>
<wicri:regionArea>Chimie ParisTech, PSL University, CNRS Institute of Chemistry for Life and Health Sciences—i-CLeHS, 11 rue Pierre et Marie Curie, F-75005 Paris</wicri:regionArea>
<placeName><region type="region" nuts="2">Île-de-France</region>
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</placeName>
</affiliation>
</author>
<author><name sortKey="Malhotra, Sanjay V" sort="Malhotra, Sanjay V" uniqKey="Malhotra S" first="Sanjay V." last="Malhotra">Sanjay V. Malhotra</name>
<affiliation><nlm:aff id="af6-molecules-24-03922">Laboratory of Synthetic Chemistry, Leidos Biomedical Research Inc., Frederick National Laboratory for Cancer Research, Frederick, MD 2170, USA;<email>smalhotra@stanford.edu</email>
</nlm:aff>
</affiliation>
<affiliation wicri:level="2"><nlm:aff id="af7-molecules-24-03922">Department of Radiation Oncology, Stanford University, 1050A Arastradero Road, A252, Palo Alto, CA 94304, USA</nlm:aff>
<country xml:lang="fr">États-Unis</country>
<wicri:regionArea>Department of Radiation Oncology, Stanford University, 1050A Arastradero Road, A252, Palo Alto, CA 94304</wicri:regionArea>
<placeName><region type="state">Californie</region>
</placeName>
</affiliation>
</author>
<author><name sortKey="Wengel, Jesper" sort="Wengel, Jesper" uniqKey="Wengel J" first="Jesper" last="Wengel">Jesper Wengel</name>
<affiliation><nlm:aff id="af9-molecules-24-03922">Nucleic Acid Center, Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, DK-5230 Odense, Denmark;<email>jwe@sdu.dk</email>
</nlm:aff>
</affiliation>
</author>
<author><name sortKey="Parmar, Virinder S" sort="Parmar, Virinder S" uniqKey="Parmar V" first="Virinder S." last="Parmar">Virinder S. Parmar</name>
<affiliation><nlm:aff id="af1-molecules-24-03922">Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India;<email>yogeshyadav77@gmail.com</email>
(Y.Y.);<email>iamvineet@gmail.com</email>
(V.K.);<email>ashokenzyme@gmail.com</email>
(A.K.P.)</nlm:aff>
</affiliation>
<affiliation><nlm:aff id="af5-molecules-24-03922">Department of Chemistry and Environmental Science, Medgar Evers College, The City University of New York, 1638 Bedford Avenue, Brooklyn, NY 11225, USA;<email>kumar.kaushik.drdo@gmail.com</email>
</nlm:aff>
</affiliation>
<affiliation><nlm:aff id="af9-molecules-24-03922">Nucleic Acid Center, Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, DK-5230 Odense, Denmark;<email>jwe@sdu.dk</email>
</nlm:aff>
</affiliation>
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<series><title level="j">Molecules</title>
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<front><div type="abstract" xml:lang="en"><p>The synthesis of novel pyrazolylnucleosides <bold>3a</bold>
–<bold>e</bold>
, <bold>4a</bold>
–<bold>e</bold>
, <bold>5a</bold>
–<bold>e</bold>
, and <bold>6a</bold>
–<bold>e</bold>
are described. The structures of the regioisomers were elucidated by using extensive NMR studies. The pyrazolylnucleosides <bold>5a</bold>
–<bold>e</bold>
and <bold>6a</bold>
–<bold>e</bold>
were screened for anticancer activities on sixty human tumor cell lines. The compound <bold>6e</bold>
showed good activity against 39 cancer cell lines. In particular, it showed significant inhibition against the lung cancer cell line Hop-92 (GI<sub>50</sub>
9.3 µM) and breast cancer cell line HS 578T (GI<sub>50</sub>
3.0 µM).</p>
</div>
</front>
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