Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines

Three series of fused pyrrolophenanthroline derivatives were designed as analogues of phenstatin and synthesized in two steps starting with 1,7-phenanthroline, 4,7-phenanthroline and 1,10-phenanthroline, respectively. Two (Compounds <b>8a</b> and <b>11c</b>) of the four compo...

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Main Authors:	Cristina Maria Al Matarneh, Roxana Maria Amarandi, Anda Mihaela Craciun, Ionel I. Mangalagiu, Gheorghita Zbancioc, Ramona Danac
Format:	Article
Language:	English
Published:	MDPI AG 2020-01-01
Series:	Molecules
Subjects:	phenanthrolines anticancer tubulin docking 3 + 2 cycloaddition phenstatin
Online Access:	https://www.mdpi.com/1420-3049/25/3/527

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spelling	doaj-48871a6278184bd48a119ecb4868ff4e2020-11-25T01:12:57ZengMDPI AGMolecules1420-30492020-01-0125352710.3390/molecules25030527molecules25030527Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused PhenanthrolinesCristina Maria Al Matarneh0Roxana Maria Amarandi1Anda Mihaela Craciun2Ionel I. Mangalagiu3Gheorghita Zbancioc4Ramona Danac5Faculty of Chemistry, Alexandru Ioan Cuza University of Iasi, 11 Carol I, 700506 Iasi, RomaniaFaculty of Chemistry, Alexandru Ioan Cuza University of Iasi, 11 Carol I, 700506 Iasi, RomaniaFaculty of Chemistry, Alexandru Ioan Cuza University of Iasi, 11 Carol I, 700506 Iasi, RomaniaFaculty of Chemistry, Alexandru Ioan Cuza University of Iasi, 11 Carol I, 700506 Iasi, RomaniaFaculty of Chemistry, Alexandru Ioan Cuza University of Iasi, 11 Carol I, 700506 Iasi, RomaniaFaculty of Chemistry, Alexandru Ioan Cuza University of Iasi, 11 Carol I, 700506 Iasi, RomaniaThree series of fused pyrrolophenanthroline derivatives were designed as analogues of phenstatin and synthesized in two steps starting with 1,7-phenanthroline, 4,7-phenanthroline and 1,10-phenanthroline, respectively. Two (Compounds <b>8a</b> and <b>11c</b>) of the four compounds tested against a panel of sixty human cancer cell lines of the National Cancer Institute (NCI) exhibited significant growth inhibition activity on several cell lines. Compound <b>11c</b> showed a broad spectrum in terms of antiproliferative efficacy with GI<sub>50</sub> values in the range of 0.296 to 250 μM. Molecular docking studies indicated that Compounds <b>8a</b> and <b>11c</b> are accommodated in the colchicine binding site of tubulin in two different ways.https://www.mdpi.com/1420-3049/25/3/527phenanthrolinesanticancertubulin docking3 + 2 cycloadditionphenstatin
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Cristina Maria Al Matarneh Roxana Maria Amarandi Anda Mihaela Craciun Ionel I. Mangalagiu Gheorghita Zbancioc Ramona Danac
spellingShingle	Cristina Maria Al Matarneh Roxana Maria Amarandi Anda Mihaela Craciun Ionel I. Mangalagiu Gheorghita Zbancioc Ramona Danac Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines Molecules phenanthrolines anticancer tubulin docking 3 + 2 cycloaddition phenstatin
author_facet	Cristina Maria Al Matarneh Roxana Maria Amarandi Anda Mihaela Craciun Ionel I. Mangalagiu Gheorghita Zbancioc Ramona Danac
author_sort	Cristina Maria Al Matarneh
title	Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines
title_short	Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines
title_full	Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines
title_fullStr	Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines
title_full_unstemmed	Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines
title_sort	design, synthesis, molecular modelling and anticancer activities of new fused phenanthrolines
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2020-01-01
description	Three series of fused pyrrolophenanthroline derivatives were designed as analogues of phenstatin and synthesized in two steps starting with 1,7-phenanthroline, 4,7-phenanthroline and 1,10-phenanthroline, respectively. Two (Compounds <b>8a</b> and <b>11c</b>) of the four compounds tested against a panel of sixty human cancer cell lines of the National Cancer Institute (NCI) exhibited significant growth inhibition activity on several cell lines. Compound <b>11c</b> showed a broad spectrum in terms of antiproliferative efficacy with GI<sub>50</sub> values in the range of 0.296 to 250 μM. Molecular docking studies indicated that Compounds <b>8a</b> and <b>11c</b> are accommodated in the colchicine binding site of tubulin in two different ways.
topic	phenanthrolines anticancer tubulin docking 3 + 2 cycloaddition phenstatin
url	https://www.mdpi.com/1420-3049/25/3/527
work_keys_str_mv	AT cristinamariaalmatarneh designsynthesismolecularmodellingandanticanceractivitiesofnewfusedphenanthrolines AT roxanamariaamarandi designsynthesismolecularmodellingandanticanceractivitiesofnewfusedphenanthrolines AT andamihaelacraciun designsynthesismolecularmodellingandanticanceractivitiesofnewfusedphenanthrolines AT ionelimangalagiu designsynthesismolecularmodellingandanticanceractivitiesofnewfusedphenanthrolines AT gheorghitazbancioc designsynthesismolecularmodellingandanticanceractivitiesofnewfusedphenanthrolines AT ramonadanac designsynthesismolecularmodellingandanticanceractivitiesofnewfusedphenanthrolines
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Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines

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