Synthesis of Spirooxindole-<em>O</em>-Naphthoquinone-Tetrazolo[1,5-<em>a</em>]Pyrimidine Hybrids as Potential Anticancer Agents

A series of novel spirooxindole-<i>O</i>-naphthoquinone-tetrazolo[1,5-<i>a</i>]pyrimidine hybrids were designed, synthesized and evaluated as potent antitumor agents. These hybrids exhibited relatively high cytotoxic activity against cancer cell line HepG2 (IC<sub>50<...

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Main Authors: Liqiang Wu, Yunxia Liu, Yazhen Li
Format: Article
Language:English
Published: MDPI AG 2018-09-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/23/9/2330
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author Liqiang Wu
Yunxia Liu
Yazhen Li
author_facet Liqiang Wu
Yunxia Liu
Yazhen Li
author_sort Liqiang Wu
collection DOAJ
description A series of novel spirooxindole-<i>O</i>-naphthoquinone-tetrazolo[1,5-<i>a</i>]pyrimidine hybrids were designed, synthesized and evaluated as potent antitumor agents. These hybrids exhibited relatively high cytotoxic activity against cancer cell line HepG2 (IC<sub>50</sub> = 2.86–36.34 μM), while normal cell line LO2 was less sensitive to these hybrids (IC<sub>50</sub> = 36.37–248.39 μM). On the whole, among all the compounds tested, compound <b>4e</b>, with a mean IC<sub>50</sub> value of 2.86 μM, was the most active. The novel hybrids may find their pharmaceutical applications after further investigations.
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institution Kabale University
issn 1420-3049
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publishDate 2018-09-01
publisher MDPI AG
record_format Article
series Molecules
spelling doaj-art-0bed47455eda41b4a249dda5f07183152024-12-13T13:30:31ZengMDPI AGMolecules1420-30492018-09-01239233010.3390/molecules23092330molecules23092330Synthesis of Spirooxindole-<em>O</em>-Naphthoquinone-Tetrazolo[1,5-<em>a</em>]Pyrimidine Hybrids as Potential Anticancer AgentsLiqiang Wu0Yunxia Liu1Yazhen Li2School of Pharmacy, Xinxiang Medical University, Xinxiang 453003, ChinaSanQuan Medical College, Xinxiang Medical University, Xinxiang 453003, ChinaSanQuan Medical College, Xinxiang Medical University, Xinxiang 453003, ChinaA series of novel spirooxindole-<i>O</i>-naphthoquinone-tetrazolo[1,5-<i>a</i>]pyrimidine hybrids were designed, synthesized and evaluated as potent antitumor agents. These hybrids exhibited relatively high cytotoxic activity against cancer cell line HepG2 (IC<sub>50</sub> = 2.86–36.34 μM), while normal cell line LO2 was less sensitive to these hybrids (IC<sub>50</sub> = 36.37–248.39 μM). On the whole, among all the compounds tested, compound <b>4e</b>, with a mean IC<sub>50</sub> value of 2.86 μM, was the most active. The novel hybrids may find their pharmaceutical applications after further investigations.https://www.mdpi.com/1420-3049/23/9/2330spirooxindole<i>O</i>-naphthoquinonehybridsantitumor activity
spellingShingle Liqiang Wu
Yunxia Liu
Yazhen Li
Synthesis of Spirooxindole-<em>O</em>-Naphthoquinone-Tetrazolo[1,5-<em>a</em>]Pyrimidine Hybrids as Potential Anticancer Agents
Molecules
spirooxindole
<i>O</i>-naphthoquinone
hybrids
antitumor activity
title Synthesis of Spirooxindole-<em>O</em>-Naphthoquinone-Tetrazolo[1,5-<em>a</em>]Pyrimidine Hybrids as Potential Anticancer Agents
title_full Synthesis of Spirooxindole-<em>O</em>-Naphthoquinone-Tetrazolo[1,5-<em>a</em>]Pyrimidine Hybrids as Potential Anticancer Agents
title_fullStr Synthesis of Spirooxindole-<em>O</em>-Naphthoquinone-Tetrazolo[1,5-<em>a</em>]Pyrimidine Hybrids as Potential Anticancer Agents
title_full_unstemmed Synthesis of Spirooxindole-<em>O</em>-Naphthoquinone-Tetrazolo[1,5-<em>a</em>]Pyrimidine Hybrids as Potential Anticancer Agents
title_short Synthesis of Spirooxindole-<em>O</em>-Naphthoquinone-Tetrazolo[1,5-<em>a</em>]Pyrimidine Hybrids as Potential Anticancer Agents
title_sort synthesis of spirooxindole em o em naphthoquinone tetrazolo 1 5 em a em pyrimidine hybrids as potential anticancer agents
topic spirooxindole
<i>O</i>-naphthoquinone
hybrids
antitumor activity
url https://www.mdpi.com/1420-3049/23/9/2330
work_keys_str_mv AT liqiangwu synthesisofspirooxindoleemoemnaphthoquinonetetrazolo15emaempyrimidinehybridsaspotentialanticanceragents
AT yunxialiu synthesisofspirooxindoleemoemnaphthoquinonetetrazolo15emaempyrimidinehybridsaspotentialanticanceragents
AT yazhenli synthesisofspirooxindoleemoemnaphthoquinonetetrazolo15emaempyrimidinehybridsaspotentialanticanceragents