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<p>Synthesis of ester derivatives of Rhein and their <em>in vitro</em> antitumor activities on cervical cancer cells (Hela)</p>

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Title Statement <p>Synthesis of ester derivatives of Rhein and their <em>in vitro</em> antitumor activities on cervical cancer cells (Hela)</p>
 
Added Entry - Uncontrolled Name Zhu, Zhi Wen; Department of Training, Tongling Vocational and Technical College, Tongling 244000, Anhui Province, China
Yang, Mei ; Department of Medicine, Tongling Vocational and Technical College, Tongling 244000, Anhui Province, China
Zhang, Jin Ping; Department of Magnetic Resonance, The People Hospital of Tongling City, Tongling 244000, Anhui Province, China
 
Uncontrolled Index Term Anticancer, Antitumor; DMAP; Ester derivatives; Esterification; Rhein
 
Summary, etc. <p style="text-align: justify;">Taking Rhein as the lead compound, ten esters of rhein were synthesized by esterification. For synthesis of smaller steric hindrance alcohols, SOCl<sub>2</sub> was used as a catalyst to synthesize methyl, ethyl and butyl esters. For lager steric hindrance alcohols, dicyclohexyl carbodiimide (DCC) was used as dehydrating agent, and 4-dimethylaminopyridine (DMAP) was used as the catalyst to synthesize isopropyl, isobutyl, tertbutyl, isoamyl, benzyl, 2-phenyl ethyl, 2-chloroethyl esters. Structural characterization of the target compounds were done using melting point, <sup>1</sup>H NMR, <sup>13</sup>C NMR and HRMS. Five out of the 10 compounds were new. All the compounds were evaluated for antitumor activities <em>in vitro</em> against Hela human cervical carcinoma cell lines. Study found that all the ten compounds showed differences in their growth inhibitory effect on tumor cells. Compound with benzyl groups improved the antitumor activity. Results showed that compound 3b exhibited maximum activity against Hela cell lines at 100 μg mL<sup>–1</sup> (IC<sub>50</sub> value) with an inhibition rate of 70%, while the derivative 3i showed the lowest inhibitory activity (IC<sub>50</sub> &lt;64.3 μg mL<sup>–1</sup>).</p>
 
Publication, Distribution, Etc. Indian Journal of Chemistry -Section A (IJCA)
2020-10-06 15:05:21
 
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http://op.niscair.res.in/index.php/IJCA/article/view/41284
 
Data Source Entry Indian Journal of Chemistry -Section A (IJCA); ##issue.vol## 59, ##issue.no## 9 (2020): INDIAN JOURNAL OF CHEMISTRY - SECTION A
 
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