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Title of Journal: Med Chem Res

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Abbravation: Medicinal Chemistry Research

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Springer US

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DOI

10.1007/s12662-014-0350-z

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ISSN

1554-8120

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Synthesis and cytotoxic evaluation of novel 23di

Authors: Santosh R Kote Ratnakar Mishra Ayesha A Khan Shankar R Thopate
Publish Date: 2013/08/30
Volume: 23, Issue: 3, Pages: 1257-1266
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Abstract

A new series of 23diOalkyl derivatives of 56Oisopropylidenelascorbic acid were synthesized using phase transfer catalysis in aqueous media These derivatives were screened for their superoxide radical scavenging activity and anticancer activity against human breast cancer cell line MCF7 leukemic cell line HL60 and cervical cell line HeLa All these derivatives exhibited enhanced scavenging effect than lascorbic acid except for the 4fluorobenzyl or 2/4chlorobenzyl alkyl group either at 3O and/or 2O position displayed prooxidant activity These prooxidant derivatives 2c–e m exhibited potent anticancer activities against all the cell lines IC50 = 2579–5721 μM However these compounds were also cytotoxic to human normal leukemic macrophages THP1 On the other hand antioxidant derivatives displayed albeit slight 2k IC50 = 5796–6345 μM but selective inhibitory effect toward all tumor cell lines Thus prooxidant and antioxidant properties can be used to predict the cytotoxic selectivity of drug against normal and cancer cellsWe thank Department of Science and Technology DST New Delhi for financial support Grant No SR/S1/OC19/2007 Professor Mukund G Kulkarni Department of Chemistry University of Pune and Dr R J Barnabas Ahmednagar College Ahmednagar for helpful discussion and suggestions Santosh R Kote thank University Grant Commission UGC New Delhi for awarding fellowship


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