Fluorescein-Labeled Thiacalix[4]arenes as Potential Theranostic Molecules: Synthesis, Self-Association, and Antitumor Activity

In this paper, a series of thiacalix[4]arenes were synthesized as potential theranostic molecules for antitumor therapy. We propose an original strategy for the regioselective functionalization of thiacalix[4]arene with a fluorescent label to obtain antiangiogenic agent mimetics. The aggregation pro...
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Gespeichert in:

Autor*in:	Alan Akhmedov [verfasserIn] Olga Terenteva [verfasserIn] Evgenia Subakaeva [verfasserIn] Pavel Zelenikhin [verfasserIn] Ramilia Shurpik [verfasserIn] Dmitriy Shurpik [verfasserIn] Pavel Padnya [verfasserIn] Ivan Stoikov [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2022

Schlagwörter:	thiacalixarene antitumor activity theranostics fluorescein quaternary ammonium salts A549

Übergeordnetes Werk:	In: Pharmaceutics - MDPI AG, 2010, 14(2022), 11, p 2340
Übergeordnetes Werk:	volume:14 ; year:2022 ; number:11, p 2340

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.3390/pharmaceutics14112340

Katalog-ID:	DOAJ025766910

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allfields	10.3390/pharmaceutics14112340 doi (DE-627)DOAJ025766910 (DE-599)DOAJ0e6e0624b8494c76862f787d48122554 DE-627 ger DE-627 rakwb eng RS1-441 Alan Akhmedov verfasserin aut Fluorescein-Labeled Thiacalix[4]arenes as Potential Theranostic Molecules: Synthesis, Self-Association, and Antitumor Activity 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In this paper, a series of thiacalix[4]arenes were synthesized as potential theranostic molecules for antitumor therapy. We propose an original strategy for the regioselective functionalization of thiacalix[4]arene with a fluorescent label to obtain antiangiogenic agent mimetics. The aggregation properties of the synthesized compounds were determined using the dynamic light scattering. The average hydrodynamic diameter of self-associates formed by the macrocycles in <i<1,3-alternate</i< conformation is larger (277–323 nm) than that of the similar macrocycle in <i<cone</i< conformation (185–262 nm). The cytotoxic action mechanism of the obtained compounds and their ability to penetrate into of human lung adenocarcinoma and human duodenal adenocarcinoma cells were established using the MTT-test and flow cytometry. thiacalix[4]arenes in <i<1,3-alternate</i< conformation did not have a strong toxic effect. The toxicity of macrocycles in <i<cone</i< conformations on <i<HuTu-80</i< and <i<A549</i< cells (IC<sub<50</sub< = 21.83–49.11 µg/mL) is shown. The resulting macrocycles are potential theranostic molecules that combine both the pharmacophore fragment for neoplasmas treatment and the fluorescent fragment for monitoring the delivery and biodistribution of nanomedicines. thiacalixarene antitumor activity theranostics fluorescein quaternary ammonium salts A549 Pharmacy and materia medica Olga Terenteva verfasserin aut Evgenia Subakaeva verfasserin aut Pavel Zelenikhin verfasserin aut Ramilia Shurpik verfasserin aut Dmitriy Shurpik verfasserin aut Pavel Padnya verfasserin aut Ivan Stoikov verfasserin aut In Pharmaceutics MDPI AG, 2010 14(2022), 11, p 2340 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:14 year:2022 number:11, p 2340 https://doi.org/10.3390/pharmaceutics14112340 kostenfrei https://doaj.org/article/0e6e0624b8494c76862f787d48122554 kostenfrei https://www.mdpi.com/1999-4923/14/11/2340 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 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_4338 GBV_ILN_4367 GBV_ILN_4700 AR 14 2022 11, p 2340
spelling	10.3390/pharmaceutics14112340 doi (DE-627)DOAJ025766910 (DE-599)DOAJ0e6e0624b8494c76862f787d48122554 DE-627 ger DE-627 rakwb eng RS1-441 Alan Akhmedov verfasserin aut Fluorescein-Labeled Thiacalix[4]arenes as Potential Theranostic Molecules: Synthesis, Self-Association, and Antitumor Activity 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In this paper, a series of thiacalix[4]arenes were synthesized as potential theranostic molecules for antitumor therapy. We propose an original strategy for the regioselective functionalization of thiacalix[4]arene with a fluorescent label to obtain antiangiogenic agent mimetics. The aggregation properties of the synthesized compounds were determined using the dynamic light scattering. The average hydrodynamic diameter of self-associates formed by the macrocycles in <i<1,3-alternate</i< conformation is larger (277–323 nm) than that of the similar macrocycle in <i<cone</i< conformation (185–262 nm). The cytotoxic action mechanism of the obtained compounds and their ability to penetrate into of human lung adenocarcinoma and human duodenal adenocarcinoma cells were established using the MTT-test and flow cytometry. thiacalix[4]arenes in <i<1,3-alternate</i< conformation did not have a strong toxic effect. The toxicity of macrocycles in <i<cone</i< conformations on <i<HuTu-80</i< and <i<A549</i< cells (IC<sub<50</sub< = 21.83–49.11 µg/mL) is shown. The resulting macrocycles are potential theranostic molecules that combine both the pharmacophore fragment for neoplasmas treatment and the fluorescent fragment for monitoring the delivery and biodistribution of nanomedicines. thiacalixarene antitumor activity theranostics fluorescein quaternary ammonium salts A549 Pharmacy and materia medica Olga Terenteva verfasserin aut Evgenia Subakaeva verfasserin aut Pavel Zelenikhin verfasserin aut Ramilia Shurpik verfasserin aut Dmitriy Shurpik verfasserin aut Pavel Padnya verfasserin aut Ivan Stoikov verfasserin aut In Pharmaceutics MDPI AG, 2010 14(2022), 11, p 2340 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:14 year:2022 number:11, p 2340 https://doi.org/10.3390/pharmaceutics14112340 kostenfrei https://doaj.org/article/0e6e0624b8494c76862f787d48122554 kostenfrei https://www.mdpi.com/1999-4923/14/11/2340 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 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_4338 GBV_ILN_4367 GBV_ILN_4700 AR 14 2022 11, p 2340
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allfieldsGer	10.3390/pharmaceutics14112340 doi (DE-627)DOAJ025766910 (DE-599)DOAJ0e6e0624b8494c76862f787d48122554 DE-627 ger DE-627 rakwb eng RS1-441 Alan Akhmedov verfasserin aut Fluorescein-Labeled Thiacalix[4]arenes as Potential Theranostic Molecules: Synthesis, Self-Association, and Antitumor Activity 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In this paper, a series of thiacalix[4]arenes were synthesized as potential theranostic molecules for antitumor therapy. We propose an original strategy for the regioselective functionalization of thiacalix[4]arene with a fluorescent label to obtain antiangiogenic agent mimetics. The aggregation properties of the synthesized compounds were determined using the dynamic light scattering. The average hydrodynamic diameter of self-associates formed by the macrocycles in <i<1,3-alternate</i< conformation is larger (277–323 nm) than that of the similar macrocycle in <i<cone</i< conformation (185–262 nm). The cytotoxic action mechanism of the obtained compounds and their ability to penetrate into of human lung adenocarcinoma and human duodenal adenocarcinoma cells were established using the MTT-test and flow cytometry. thiacalix[4]arenes in <i<1,3-alternate</i< conformation did not have a strong toxic effect. The toxicity of macrocycles in <i<cone</i< conformations on <i<HuTu-80</i< and <i<A549</i< cells (IC<sub<50</sub< = 21.83–49.11 µg/mL) is shown. The resulting macrocycles are potential theranostic molecules that combine both the pharmacophore fragment for neoplasmas treatment and the fluorescent fragment for monitoring the delivery and biodistribution of nanomedicines. thiacalixarene antitumor activity theranostics fluorescein quaternary ammonium salts A549 Pharmacy and materia medica Olga Terenteva verfasserin aut Evgenia Subakaeva verfasserin aut Pavel Zelenikhin verfasserin aut Ramilia Shurpik verfasserin aut Dmitriy Shurpik verfasserin aut Pavel Padnya verfasserin aut Ivan Stoikov verfasserin aut In Pharmaceutics MDPI AG, 2010 14(2022), 11, p 2340 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:14 year:2022 number:11, p 2340 https://doi.org/10.3390/pharmaceutics14112340 kostenfrei https://doaj.org/article/0e6e0624b8494c76862f787d48122554 kostenfrei https://www.mdpi.com/1999-4923/14/11/2340 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 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_4338 GBV_ILN_4367 GBV_ILN_4700 AR 14 2022 11, p 2340
allfieldsSound	10.3390/pharmaceutics14112340 doi (DE-627)DOAJ025766910 (DE-599)DOAJ0e6e0624b8494c76862f787d48122554 DE-627 ger DE-627 rakwb eng RS1-441 Alan Akhmedov verfasserin aut Fluorescein-Labeled Thiacalix[4]arenes as Potential Theranostic Molecules: Synthesis, Self-Association, and Antitumor Activity 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier In this paper, a series of thiacalix[4]arenes were synthesized as potential theranostic molecules for antitumor therapy. We propose an original strategy for the regioselective functionalization of thiacalix[4]arene with a fluorescent label to obtain antiangiogenic agent mimetics. The aggregation properties of the synthesized compounds were determined using the dynamic light scattering. The average hydrodynamic diameter of self-associates formed by the macrocycles in <i<1,3-alternate</i< conformation is larger (277–323 nm) than that of the similar macrocycle in <i<cone</i< conformation (185–262 nm). The cytotoxic action mechanism of the obtained compounds and their ability to penetrate into of human lung adenocarcinoma and human duodenal adenocarcinoma cells were established using the MTT-test and flow cytometry. thiacalix[4]arenes in <i<1,3-alternate</i< conformation did not have a strong toxic effect. The toxicity of macrocycles in <i<cone</i< conformations on <i<HuTu-80</i< and <i<A549</i< cells (IC<sub<50</sub< = 21.83–49.11 µg/mL) is shown. The resulting macrocycles are potential theranostic molecules that combine both the pharmacophore fragment for neoplasmas treatment and the fluorescent fragment for monitoring the delivery and biodistribution of nanomedicines. thiacalixarene antitumor activity theranostics fluorescein quaternary ammonium salts A549 Pharmacy and materia medica Olga Terenteva verfasserin aut Evgenia Subakaeva verfasserin aut Pavel Zelenikhin verfasserin aut Ramilia Shurpik verfasserin aut Dmitriy Shurpik verfasserin aut Pavel Padnya verfasserin aut Ivan Stoikov verfasserin aut In Pharmaceutics MDPI AG, 2010 14(2022), 11, p 2340 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:14 year:2022 number:11, p 2340 https://doi.org/10.3390/pharmaceutics14112340 kostenfrei https://doaj.org/article/0e6e0624b8494c76862f787d48122554 kostenfrei https://www.mdpi.com/1999-4923/14/11/2340 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 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_4338 GBV_ILN_4367 GBV_ILN_4700 AR 14 2022 11, p 2340
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authorswithroles_txt_mv	Alan Akhmedov @@aut@@ Olga Terenteva @@aut@@ Evgenia Subakaeva @@aut@@ Pavel Zelenikhin @@aut@@ Ramilia Shurpik @@aut@@ Dmitriy Shurpik @@aut@@ Pavel Padnya @@aut@@ Ivan Stoikov @@aut@@
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callnumber-first	R - Medicine
author	Alan Akhmedov
spellingShingle	Alan Akhmedov misc RS1-441 misc thiacalixarene misc antitumor activity misc theranostics misc fluorescein misc quaternary ammonium salts misc A549 misc Pharmacy and materia medica Fluorescein-Labeled Thiacalix[4]arenes as Potential Theranostic Molecules: Synthesis, Self-Association, and Antitumor Activity
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topic_title	RS1-441 Fluorescein-Labeled Thiacalix[4]arenes as Potential Theranostic Molecules: Synthesis, Self-Association, and Antitumor Activity thiacalixarene antitumor activity theranostics fluorescein quaternary ammonium salts A549
topic	misc RS1-441 misc thiacalixarene misc antitumor activity misc theranostics misc fluorescein misc quaternary ammonium salts misc A549 misc Pharmacy and materia medica
topic_unstemmed	misc RS1-441 misc thiacalixarene misc antitumor activity misc theranostics misc fluorescein misc quaternary ammonium salts misc A549 misc Pharmacy and materia medica
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title	Fluorescein-Labeled Thiacalix[4]arenes as Potential Theranostic Molecules: Synthesis, Self-Association, and Antitumor Activity
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title_full	Fluorescein-Labeled Thiacalix[4]arenes as Potential Theranostic Molecules: Synthesis, Self-Association, and Antitumor Activity
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title_sort	fluorescein-labeled thiacalix[4]arenes as potential theranostic molecules: synthesis, self-association, and antitumor activity
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title_auth	Fluorescein-Labeled Thiacalix[4]arenes as Potential Theranostic Molecules: Synthesis, Self-Association, and Antitumor Activity
abstract	In this paper, a series of thiacalix[4]arenes were synthesized as potential theranostic molecules for antitumor therapy. We propose an original strategy for the regioselective functionalization of thiacalix[4]arene with a fluorescent label to obtain antiangiogenic agent mimetics. The aggregation properties of the synthesized compounds were determined using the dynamic light scattering. The average hydrodynamic diameter of self-associates formed by the macrocycles in <i<1,3-alternate</i< conformation is larger (277–323 nm) than that of the similar macrocycle in <i<cone</i< conformation (185–262 nm). The cytotoxic action mechanism of the obtained compounds and their ability to penetrate into of human lung adenocarcinoma and human duodenal adenocarcinoma cells were established using the MTT-test and flow cytometry. thiacalix[4]arenes in <i<1,3-alternate</i< conformation did not have a strong toxic effect. The toxicity of macrocycles in <i<cone</i< conformations on <i<HuTu-80</i< and <i<A549</i< cells (IC<sub<50</sub< = 21.83–49.11 µg/mL) is shown. The resulting macrocycles are potential theranostic molecules that combine both the pharmacophore fragment for neoplasmas treatment and the fluorescent fragment for monitoring the delivery and biodistribution of nanomedicines.
abstractGer	In this paper, a series of thiacalix[4]arenes were synthesized as potential theranostic molecules for antitumor therapy. We propose an original strategy for the regioselective functionalization of thiacalix[4]arene with a fluorescent label to obtain antiangiogenic agent mimetics. The aggregation properties of the synthesized compounds were determined using the dynamic light scattering. The average hydrodynamic diameter of self-associates formed by the macrocycles in <i<1,3-alternate</i< conformation is larger (277–323 nm) than that of the similar macrocycle in <i<cone</i< conformation (185–262 nm). The cytotoxic action mechanism of the obtained compounds and their ability to penetrate into of human lung adenocarcinoma and human duodenal adenocarcinoma cells were established using the MTT-test and flow cytometry. thiacalix[4]arenes in <i<1,3-alternate</i< conformation did not have a strong toxic effect. The toxicity of macrocycles in <i<cone</i< conformations on <i<HuTu-80</i< and <i<A549</i< cells (IC<sub<50</sub< = 21.83–49.11 µg/mL) is shown. The resulting macrocycles are potential theranostic molecules that combine both the pharmacophore fragment for neoplasmas treatment and the fluorescent fragment for monitoring the delivery and biodistribution of nanomedicines.
abstract_unstemmed	In this paper, a series of thiacalix[4]arenes were synthesized as potential theranostic molecules for antitumor therapy. We propose an original strategy for the regioselective functionalization of thiacalix[4]arene with a fluorescent label to obtain antiangiogenic agent mimetics. The aggregation properties of the synthesized compounds were determined using the dynamic light scattering. The average hydrodynamic diameter of self-associates formed by the macrocycles in <i<1,3-alternate</i< conformation is larger (277–323 nm) than that of the similar macrocycle in <i<cone</i< conformation (185–262 nm). The cytotoxic action mechanism of the obtained compounds and their ability to penetrate into of human lung adenocarcinoma and human duodenal adenocarcinoma cells were established using the MTT-test and flow cytometry. thiacalix[4]arenes in <i<1,3-alternate</i< conformation did not have a strong toxic effect. The toxicity of macrocycles in <i<cone</i< conformations on <i<HuTu-80</i< and <i<A549</i< cells (IC<sub<50</sub< = 21.83–49.11 µg/mL) is shown. The resulting macrocycles are potential theranostic molecules that combine both the pharmacophore fragment for neoplasmas treatment and the fluorescent fragment for monitoring the delivery and biodistribution of nanomedicines.
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title_short	Fluorescein-Labeled Thiacalix[4]arenes as Potential Theranostic Molecules: Synthesis, Self-Association, and Antitumor Activity
url	https://doi.org/10.3390/pharmaceutics14112340 https://doaj.org/article/0e6e0624b8494c76862f787d48122554 https://www.mdpi.com/1999-4923/14/11/2340 https://doaj.org/toc/1999-4923
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up_date	2024-07-03T16:59:06.357Z
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We propose an original strategy for the regioselective functionalization of thiacalix[4]arene with a fluorescent label to obtain antiangiogenic agent mimetics. The aggregation properties of the synthesized compounds were determined using the dynamic light scattering. The average hydrodynamic diameter of self-associates formed by the macrocycles in <i<1,3-alternate</i< conformation is larger (277–323 nm) than that of the similar macrocycle in <i<cone</i< conformation (185–262 nm). The cytotoxic action mechanism of the obtained compounds and their ability to penetrate into of human lung adenocarcinoma and human duodenal adenocarcinoma cells were established using the MTT-test and flow cytometry. thiacalix[4]arenes in <i<1,3-alternate</i< conformation did not have a strong toxic effect. The toxicity of macrocycles in <i<cone</i< conformations on <i<HuTu-80</i< and <i<A549</i< cells (IC<sub<50</sub< = 21.83–49.11 µg/mL) is shown. 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Fluorescein-Labeled Thiacalix[4]arenes as Potential Theranostic Molecules: Synthesis, Self-Association, and Antitumor Activity

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