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INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH

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IJPR included in UGC-Approved List of Journals - Ref. No. is SL. No. 4812 & J. No. 63703

Published by : Advanced Scientific Research
ISSN
0975-2366
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IJPR 9[3] July - September 2017 Special Issue

July - September 9[3] 2017

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Synthesis of New oxazine and oxazocine derivatives and Evaluation of their Antiproliferative Potency against Different Cancer Cell Lines

Author: KHADIGA AHMED, HANAA A. TAWFIK, NAGWA M. FAWZY, SHWEEKAR I. EL NAEM, MAGDE S. ALY
Abstract: A new method was proceeding the synthesis of new oxazocine derivatives 4a, by a condensation reaction of: aldehyde 1, Meldrum’s acid 2, and isocyanate derivatives 3a, b in dichloromethane at room temperature. A novel isocyanate-based four-component reaction between an aldehyde 1, Meldrum’s acid 2, an isocyanate derivatives 10a-c and an aromatic phenol derivative 9a, b/ and or p-anisidine 9c was provided oxazocine derivatives 11a-i. A novel one-pot procedure of three-component reaction for the preparation oxazine-derivatives 13a-d was described by heating a mixture of an anthranilic acid, aldehyde 1, and an isocyanate derivatives 12a-d in methanol. All of the newly prepared compounds were evaluated as anti-cancer activity against hepatocellular carcinoma cell line HEPG2, breast carcinoma cell line MCF-7, prostate carcinoma cell line PC3. Anticancer activity results indicated that the synthesized products 4b, 11b, 13b, 11e and 11i showed growth inhibition activity against two of the tested cell lines (HEPG-2 and PC3) but with changing intensities extents against Doxorubicin as a reference anticancer drug. Our results also showed that all compounds did not have any activity against human breast MCF-7 cells. The results yielded a theoretical reference for the exploration of new anti-cancer agents and may be helpful in designing drugs for chemotherapy.
Keyword: Isocyanate, isothiocyanates oxazocine, multi-component reactions, oxazine, cytotoxicity, anticancer activity, human cancer cell lines.
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