Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors

A series of celastrol derivatives were synthesized and evaluated as hypoxia-inducible factor-1α (HIF-1α) inhibitors. Among these compounds, 4b and 4d appeared to have high HIF-1α inhibitory activity of 2.97 and 2.99 μM $ IC_{50} $ values respectively. The cytotoxicity of these compounds was also ass...
Ausführliche Beschreibung

Gespeichert in:

Autor*in:	Ren, Xiaoqun [verfasserIn] Cui, Linlin Wang, Yang Li, Huayun Shen, Guanghuan

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2022

Schlagwörter:	HIF-1α celastrol cytotoxicity Hep3B cells

Anmerkung:	© Springer Science+Business Media, LLC, part of Springer Nature 2022. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law.

Übergeordnetes Werk:	Enthalten in: Chemistry of natural compounds - New York, NY [u.a.] : Consultants Bureau, 1965, 58(2022), 6 vom: Nov., Seite 1075-1078
Übergeordnetes Werk:	volume:58 ; year:2022 ; number:6 ; month:11 ; pages:1075-1078

Links:	Volltext

DOI / URN:	10.1007/s10600-022-03870-z

Katalog-ID:	SPR048662798

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520			\|a A series of celastrol derivatives were synthesized and evaluated as hypoxia-inducible factor-1α (HIF-1α) inhibitors. Among these compounds, 4b and 4d appeared to have high HIF-1α inhibitory activity of 2.97 and 2.99 μM $ IC_{50} $ values respectively. The cytotoxicity of these compounds was also assessed in Hep3B cells using the MTT assay, and no compounds showed any appreciable cytotoxic activity ($ IC_{50} $ > 50 μmol/L).
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912			\|a GBV_ILN_152
912			\|a GBV_ILN_161
912			\|a GBV_ILN_170
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912			\|a GBV_ILN_187
912			\|a GBV_ILN_206
912			\|a GBV_ILN_213
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912			\|a GBV_ILN_230
912			\|a GBV_ILN_250
912			\|a GBV_ILN_281
912			\|a GBV_ILN_285
912			\|a GBV_ILN_293
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912			\|a GBV_ILN_702
912			\|a GBV_ILN_2001
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912			\|a GBV_ILN_2005
912			\|a GBV_ILN_2006
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912			\|a GBV_ILN_2026
912			\|a GBV_ILN_2027
912			\|a GBV_ILN_2031
912			\|a GBV_ILN_2034
912			\|a GBV_ILN_2037
912			\|a GBV_ILN_2038
912			\|a GBV_ILN_2039
912			\|a GBV_ILN_2044
912			\|a GBV_ILN_2048
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912			\|a GBV_ILN_2110
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allfields	10.1007/s10600-022-03870-z doi (DE-627)SPR048662798 (SPR)s10600-022-03870-z-e DE-627 ger DE-627 rakwb eng Ren, Xiaoqun verfasserin aut Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier © Springer Science+Business Media, LLC, part of Springer Nature 2022. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law. A series of celastrol derivatives were synthesized and evaluated as hypoxia-inducible factor-1α (HIF-1α) inhibitors. Among these compounds, 4b and 4d appeared to have high HIF-1α inhibitory activity of 2.97 and 2.99 μM $ IC_{50} $ values respectively. The cytotoxicity of these compounds was also assessed in Hep3B cells using the MTT assay, and no compounds showed any appreciable cytotoxic activity ($ IC_{50} $ > 50 μmol/L). HIF-1α (dpeaa)DE-He213 celastrol (dpeaa)DE-He213 cytotoxicity (dpeaa)DE-He213 Hep3B cells (dpeaa)DE-He213 Cui, Linlin aut Wang, Yang aut Li, Huayun aut Shen, Guanghuan aut Enthalten in Chemistry of natural compounds New York, NY [u.a.] : Consultants Bureau, 1965 58(2022), 6 vom: Nov., Seite 1075-1078 (DE-627)325568618 (DE-600)2037133-0 1573-8388 nnns volume:58 year:2022 number:6 month:11 pages:1075-1078 https://dx.doi.org/10.1007/s10600-022-03870-z lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_152 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4328 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 AR 58 2022 6 11 1075-1078
spelling	10.1007/s10600-022-03870-z doi (DE-627)SPR048662798 (SPR)s10600-022-03870-z-e DE-627 ger DE-627 rakwb eng Ren, Xiaoqun verfasserin aut Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier © Springer Science+Business Media, LLC, part of Springer Nature 2022. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law. A series of celastrol derivatives were synthesized and evaluated as hypoxia-inducible factor-1α (HIF-1α) inhibitors. Among these compounds, 4b and 4d appeared to have high HIF-1α inhibitory activity of 2.97 and 2.99 μM $ IC_{50} $ values respectively. The cytotoxicity of these compounds was also assessed in Hep3B cells using the MTT assay, and no compounds showed any appreciable cytotoxic activity ($ IC_{50} $ > 50 μmol/L). HIF-1α (dpeaa)DE-He213 celastrol (dpeaa)DE-He213 cytotoxicity (dpeaa)DE-He213 Hep3B cells (dpeaa)DE-He213 Cui, Linlin aut Wang, Yang aut Li, Huayun aut Shen, Guanghuan aut Enthalten in Chemistry of natural compounds New York, NY [u.a.] : Consultants Bureau, 1965 58(2022), 6 vom: Nov., Seite 1075-1078 (DE-627)325568618 (DE-600)2037133-0 1573-8388 nnns volume:58 year:2022 number:6 month:11 pages:1075-1078 https://dx.doi.org/10.1007/s10600-022-03870-z lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_152 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4328 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 AR 58 2022 6 11 1075-1078
allfields_unstemmed	10.1007/s10600-022-03870-z doi (DE-627)SPR048662798 (SPR)s10600-022-03870-z-e DE-627 ger DE-627 rakwb eng Ren, Xiaoqun verfasserin aut Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier © Springer Science+Business Media, LLC, part of Springer Nature 2022. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law. A series of celastrol derivatives were synthesized and evaluated as hypoxia-inducible factor-1α (HIF-1α) inhibitors. Among these compounds, 4b and 4d appeared to have high HIF-1α inhibitory activity of 2.97 and 2.99 μM $ IC_{50} $ values respectively. The cytotoxicity of these compounds was also assessed in Hep3B cells using the MTT assay, and no compounds showed any appreciable cytotoxic activity ($ IC_{50} $ > 50 μmol/L). HIF-1α (dpeaa)DE-He213 celastrol (dpeaa)DE-He213 cytotoxicity (dpeaa)DE-He213 Hep3B cells (dpeaa)DE-He213 Cui, Linlin aut Wang, Yang aut Li, Huayun aut Shen, Guanghuan aut Enthalten in Chemistry of natural compounds New York, NY [u.a.] : Consultants Bureau, 1965 58(2022), 6 vom: Nov., Seite 1075-1078 (DE-627)325568618 (DE-600)2037133-0 1573-8388 nnns volume:58 year:2022 number:6 month:11 pages:1075-1078 https://dx.doi.org/10.1007/s10600-022-03870-z lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_152 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4328 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 AR 58 2022 6 11 1075-1078
allfieldsGer	10.1007/s10600-022-03870-z doi (DE-627)SPR048662798 (SPR)s10600-022-03870-z-e DE-627 ger DE-627 rakwb eng Ren, Xiaoqun verfasserin aut Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier © Springer Science+Business Media, LLC, part of Springer Nature 2022. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law. A series of celastrol derivatives were synthesized and evaluated as hypoxia-inducible factor-1α (HIF-1α) inhibitors. Among these compounds, 4b and 4d appeared to have high HIF-1α inhibitory activity of 2.97 and 2.99 μM $ IC_{50} $ values respectively. The cytotoxicity of these compounds was also assessed in Hep3B cells using the MTT assay, and no compounds showed any appreciable cytotoxic activity ($ IC_{50} $ > 50 μmol/L). HIF-1α (dpeaa)DE-He213 celastrol (dpeaa)DE-He213 cytotoxicity (dpeaa)DE-He213 Hep3B cells (dpeaa)DE-He213 Cui, Linlin aut Wang, Yang aut Li, Huayun aut Shen, Guanghuan aut Enthalten in Chemistry of natural compounds New York, NY [u.a.] : Consultants Bureau, 1965 58(2022), 6 vom: Nov., Seite 1075-1078 (DE-627)325568618 (DE-600)2037133-0 1573-8388 nnns volume:58 year:2022 number:6 month:11 pages:1075-1078 https://dx.doi.org/10.1007/s10600-022-03870-z lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_152 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4328 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 AR 58 2022 6 11 1075-1078
allfieldsSound	10.1007/s10600-022-03870-z doi (DE-627)SPR048662798 (SPR)s10600-022-03870-z-e DE-627 ger DE-627 rakwb eng Ren, Xiaoqun verfasserin aut Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier © Springer Science+Business Media, LLC, part of Springer Nature 2022. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law. A series of celastrol derivatives were synthesized and evaluated as hypoxia-inducible factor-1α (HIF-1α) inhibitors. Among these compounds, 4b and 4d appeared to have high HIF-1α inhibitory activity of 2.97 and 2.99 μM $ IC_{50} $ values respectively. The cytotoxicity of these compounds was also assessed in Hep3B cells using the MTT assay, and no compounds showed any appreciable cytotoxic activity ($ IC_{50} $ > 50 μmol/L). HIF-1α (dpeaa)DE-He213 celastrol (dpeaa)DE-He213 cytotoxicity (dpeaa)DE-He213 Hep3B cells (dpeaa)DE-He213 Cui, Linlin aut Wang, Yang aut Li, Huayun aut Shen, Guanghuan aut Enthalten in Chemistry of natural compounds New York, NY [u.a.] : Consultants Bureau, 1965 58(2022), 6 vom: Nov., Seite 1075-1078 (DE-627)325568618 (DE-600)2037133-0 1573-8388 nnns volume:58 year:2022 number:6 month:11 pages:1075-1078 https://dx.doi.org/10.1007/s10600-022-03870-z lizenzpflichtig Volltext GBV_USEFLAG_A SYSFLAG_A GBV_SPRINGER SSG-OLC-PHA GBV_ILN_11 GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_32 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_74 GBV_ILN_90 GBV_ILN_95 GBV_ILN_100 GBV_ILN_101 GBV_ILN_105 GBV_ILN_110 GBV_ILN_120 GBV_ILN_138 GBV_ILN_150 GBV_ILN_151 GBV_ILN_152 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_187 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_250 GBV_ILN_281 GBV_ILN_285 GBV_ILN_293 GBV_ILN_370 GBV_ILN_602 GBV_ILN_636 GBV_ILN_702 GBV_ILN_2001 GBV_ILN_2003 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2008 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2015 GBV_ILN_2020 GBV_ILN_2021 GBV_ILN_2025 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2031 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2039 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2064 GBV_ILN_2065 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2093 GBV_ILN_2106 GBV_ILN_2107 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2112 GBV_ILN_2113 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2129 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2188 GBV_ILN_2190 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2446 GBV_ILN_2470 GBV_ILN_2472 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_2548 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4246 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4328 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4393 GBV_ILN_4700 AR 58 2022 6 11 1075-1078
language	English
source	Enthalten in Chemistry of natural compounds 58(2022), 6 vom: Nov., Seite 1075-1078 volume:58 year:2022 number:6 month:11 pages:1075-1078
sourceStr	Enthalten in Chemistry of natural compounds 58(2022), 6 vom: Nov., Seite 1075-1078 volume:58 year:2022 number:6 month:11 pages:1075-1078
format_phy_str_mv	Article
institution	findex.gbv.de
topic_facet	HIF-1α celastrol cytotoxicity Hep3B cells
isfreeaccess_bool	false
container_title	Chemistry of natural compounds
authorswithroles_txt_mv	Ren, Xiaoqun @@aut@@ Cui, Linlin @@aut@@ Wang, Yang @@aut@@ Li, Huayun @@aut@@ Shen, Guanghuan @@aut@@
publishDateDaySort_date	2022-11-01T00:00:00Z
hierarchy_top_id	325568618
id	SPR048662798
language_de	englisch
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author	Ren, Xiaoqun
spellingShingle	Ren, Xiaoqun misc HIF-1α misc celastrol misc cytotoxicity misc Hep3B cells Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors
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topic_title	Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors HIF-1α (dpeaa)DE-He213 celastrol (dpeaa)DE-He213 cytotoxicity (dpeaa)DE-He213 Hep3B cells (dpeaa)DE-He213
topic	misc HIF-1α misc celastrol misc cytotoxicity misc Hep3B cells
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title	Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors
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title_full	Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors
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author_browse	Ren, Xiaoqun Cui, Linlin Wang, Yang Li, Huayun Shen, Guanghuan
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author-letter	Ren, Xiaoqun
doi_str_mv	10.1007/s10600-022-03870-z
title_sort	synthesis and evaluation of celastrol derivatives as hif-1α inhibitors
title_auth	Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors
abstract	A series of celastrol derivatives were synthesized and evaluated as hypoxia-inducible factor-1α (HIF-1α) inhibitors. Among these compounds, 4b and 4d appeared to have high HIF-1α inhibitory activity of 2.97 and 2.99 μM $ IC_{50} $ values respectively. The cytotoxicity of these compounds was also assessed in Hep3B cells using the MTT assay, and no compounds showed any appreciable cytotoxic activity ($ IC_{50} $ > 50 μmol/L). © Springer Science+Business Media, LLC, part of Springer Nature 2022. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law.
abstractGer	A series of celastrol derivatives were synthesized and evaluated as hypoxia-inducible factor-1α (HIF-1α) inhibitors. Among these compounds, 4b and 4d appeared to have high HIF-1α inhibitory activity of 2.97 and 2.99 μM $ IC_{50} $ values respectively. The cytotoxicity of these compounds was also assessed in Hep3B cells using the MTT assay, and no compounds showed any appreciable cytotoxic activity ($ IC_{50} $ > 50 μmol/L). © Springer Science+Business Media, LLC, part of Springer Nature 2022. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law.
abstract_unstemmed	A series of celastrol derivatives were synthesized and evaluated as hypoxia-inducible factor-1α (HIF-1α) inhibitors. Among these compounds, 4b and 4d appeared to have high HIF-1α inhibitory activity of 2.97 and 2.99 μM $ IC_{50} $ values respectively. The cytotoxicity of these compounds was also assessed in Hep3B cells using the MTT assay, and no compounds showed any appreciable cytotoxic activity ($ IC_{50} $ > 50 μmol/L). © Springer Science+Business Media, LLC, part of Springer Nature 2022. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law.
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title_short	Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors
url	https://dx.doi.org/10.1007/s10600-022-03870-z
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author2	Cui, Linlin Wang, Yang Li, Huayun Shen, Guanghuan
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doi_str	10.1007/s10600-022-03870-z
up_date	2024-07-03T20:40:38.362Z
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Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors

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