In vitro cytotoxicity and apoptotic inducing activity of the synthesized 4-aryl-4H-chromenes derivatives against human cancer cell lines

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Main Authors: Mohagheghi MA, Divsalar K, Khoshzaban A, Safavi M, Hidarykeshel S, Foroumadi A, Rajabalian S, Mahmoodi M
Format: Article
Language:fas
Published: Tehran University of Medical Sciences 2009-09-01
Series:Tehran University Medical Journal
Subjects:
Online Access:http://journals.tums.ac.ir/PdfMed.aspx?pdf_med=/upload_files/pdf/14563.pdf&manuscript_id=14563
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author Mohagheghi MA
Divsalar K
Khoshzaban A
Safavi M
Hidarykeshel S
Foroumadi A
Rajabalian S
Mahmoodi M
author_facet Mohagheghi MA
Divsalar K
Khoshzaban A
Safavi M
Hidarykeshel S
Foroumadi A
Rajabalian S
Mahmoodi M
author_sort Mohagheghi MA
collection DOAJ
description "n Normal 0 false false false EN-US X-NONE AR-SA MicrosoftInternetExplorer4 /* Style Definitions */ table.MsoNormalTable {mso-style-name:"Table Normal"; mso-tstyle-rowband-size:0; mso-tstyle-colband-size:0; mso-style-noshow:yes; mso-style-priority:99; mso-style-qformat:yes; mso-style-parent:""; mso-padding-alt:0in 5.4pt 0in 5.4pt; mso-para-margin:0in; mso-para-margin-bottom:.0001pt; mso-pagination:widow-orphan; font-size:11.0pt; font-family:"Calibri","sans-serif"; mso-ascii-font-family:Calibri; mso-ascii-theme-font:minor-latin; mso-fareast-font-family:"Times New Roman"; mso-fareast-theme-font:minor-fareast; mso-hansi-font-family:Calibri; mso-hansi-theme-font:minor-latin; mso-bidi-font-family:Arial; mso-bidi-theme-font:minor-bidi;} Background: 4-Aryl-4H-chromenes are novel anticancer agents which induce apoptosis in cancer cells. These compounds were found to induce apoptosis by targeting the tubulin/microtubule system in cell proliferation process. The aim of this study was to report cyototoxic and apoptosis inducing activities of a new series of synthesized 4-aryl-4H-chromenes compounds."n"n Methods: The in vitro cytotoxic activity of the synthesized 4-aryl-4H-chromenes was investigated against a paned of human cancer cell lines including MCF-7 (breast carcinoma), A549 (lung carcinoma), HEPG-2 (liver carcinoma), SW-480 (colon adenocarcinoma), U87-MG (glioblastoma), 1321N1 (astrocytoma), and DAOY (medulloblastoma). The percentage of growth inhibitory activity was evaluated using MTT colorimetric assay versus controls not treated with test derivatives. The data for etoposide, a well known anticancer drug, was included for comparison. For each compound, the 50% inhibitory concentration (IC50) were determined. Apoptosis inducing activity were assessed by DAPI staining."n"n Results: Preliminary screening showed that those chromenes analogs bearing phenyl-isoxazole-3-yl substitution or the derivatives containing methoxyphenyl in chromene ring exhibited cytotoxic and apoptotic inducing activity comparable with or even superior than the reference drug, etoposide. The compounds without this type of substitution have lower activity. "n"nConclusions: Replacement of 3, 4, 5-trimethoxyphenyl group with thiazol ring in the synthesized derivatives reduced the cytotoxic activity. However, the derivatives with phenyl-isoxazole analogue showed potent cytotoxic and apoptotic inducing activity.
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spelling doaj.art-19b0b671df2748d282b7117d4970b4b22022-12-22T02:10:26ZfasTehran University of Medical SciencesTehran University Medical Journal1683-17641735-73222009-09-01676387392In vitro cytotoxicity and apoptotic inducing activity of the synthesized 4-aryl-4H-chromenes derivatives against human cancer cell linesMohagheghi MADivsalar KKhoshzaban ASafavi MHidarykeshel SForoumadi ARajabalian SMahmoodi M"n Normal 0 false false false EN-US X-NONE AR-SA MicrosoftInternetExplorer4 /* Style Definitions */ table.MsoNormalTable {mso-style-name:"Table Normal"; mso-tstyle-rowband-size:0; mso-tstyle-colband-size:0; mso-style-noshow:yes; mso-style-priority:99; mso-style-qformat:yes; mso-style-parent:""; mso-padding-alt:0in 5.4pt 0in 5.4pt; mso-para-margin:0in; mso-para-margin-bottom:.0001pt; mso-pagination:widow-orphan; font-size:11.0pt; font-family:"Calibri","sans-serif"; mso-ascii-font-family:Calibri; mso-ascii-theme-font:minor-latin; mso-fareast-font-family:"Times New Roman"; mso-fareast-theme-font:minor-fareast; mso-hansi-font-family:Calibri; mso-hansi-theme-font:minor-latin; mso-bidi-font-family:Arial; mso-bidi-theme-font:minor-bidi;} Background: 4-Aryl-4H-chromenes are novel anticancer agents which induce apoptosis in cancer cells. These compounds were found to induce apoptosis by targeting the tubulin/microtubule system in cell proliferation process. The aim of this study was to report cyototoxic and apoptosis inducing activities of a new series of synthesized 4-aryl-4H-chromenes compounds."n"n Methods: The in vitro cytotoxic activity of the synthesized 4-aryl-4H-chromenes was investigated against a paned of human cancer cell lines including MCF-7 (breast carcinoma), A549 (lung carcinoma), HEPG-2 (liver carcinoma), SW-480 (colon adenocarcinoma), U87-MG (glioblastoma), 1321N1 (astrocytoma), and DAOY (medulloblastoma). The percentage of growth inhibitory activity was evaluated using MTT colorimetric assay versus controls not treated with test derivatives. The data for etoposide, a well known anticancer drug, was included for comparison. For each compound, the 50% inhibitory concentration (IC50) were determined. Apoptosis inducing activity were assessed by DAPI staining."n"n Results: Preliminary screening showed that those chromenes analogs bearing phenyl-isoxazole-3-yl substitution or the derivatives containing methoxyphenyl in chromene ring exhibited cytotoxic and apoptotic inducing activity comparable with or even superior than the reference drug, etoposide. The compounds without this type of substitution have lower activity. "n"nConclusions: Replacement of 3, 4, 5-trimethoxyphenyl group with thiazol ring in the synthesized derivatives reduced the cytotoxic activity. However, the derivatives with phenyl-isoxazole analogue showed potent cytotoxic and apoptotic inducing activity.http://journals.tums.ac.ir/PdfMed.aspx?pdf_med=/upload_files/pdf/14563.pdf&manuscript_id=145634-aryl-4H-chromenescyototoxic activityapoptosis
spellingShingle Mohagheghi MA
Divsalar K
Khoshzaban A
Safavi M
Hidarykeshel S
Foroumadi A
Rajabalian S
Mahmoodi M
In vitro cytotoxicity and apoptotic inducing activity of the synthesized 4-aryl-4H-chromenes derivatives against human cancer cell lines
Tehran University Medical Journal
4-aryl-4H-chromenes
cyototoxic activity
apoptosis
title In vitro cytotoxicity and apoptotic inducing activity of the synthesized 4-aryl-4H-chromenes derivatives against human cancer cell lines
title_full In vitro cytotoxicity and apoptotic inducing activity of the synthesized 4-aryl-4H-chromenes derivatives against human cancer cell lines
title_fullStr In vitro cytotoxicity and apoptotic inducing activity of the synthesized 4-aryl-4H-chromenes derivatives against human cancer cell lines
title_full_unstemmed In vitro cytotoxicity and apoptotic inducing activity of the synthesized 4-aryl-4H-chromenes derivatives against human cancer cell lines
title_short In vitro cytotoxicity and apoptotic inducing activity of the synthesized 4-aryl-4H-chromenes derivatives against human cancer cell lines
title_sort in vitro cytotoxicity and apoptotic inducing activity of the synthesized 4 aryl 4h chromenes derivatives against human cancer cell lines
topic 4-aryl-4H-chromenes
cyototoxic activity
apoptosis
url http://journals.tums.ac.ir/PdfMed.aspx?pdf_med=/upload_files/pdf/14563.pdf&manuscript_id=14563
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AT foroumadia invitrocytotoxicityandapoptoticinducingactivityofthesynthesized4aryl4hchromenesderivativesagainsthumancancercelllines
AT rajabalians invitrocytotoxicityandapoptoticinducingactivityofthesynthesized4aryl4hchromenesderivativesagainsthumancancercelllines
AT mahmoodim invitrocytotoxicityandapoptoticinducingactivityofthesynthesized4aryl4hchromenesderivativesagainsthumancancercelllines