Cytotoxicity and gene expression profiles of novel synthesized steroid derivatives as chemotherapeutic anti-breast cancer agents

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dc.AffiliationOctober University for modern sciences and Arts (MSA)
dc.contributor.authorElmegeed G.A.
dc.contributor.authorKhalil W.K.B.
dc.contributor.authorMohareb R.M.
dc.contributor.authorAhmed H.H.
dc.contributor.authorAbd-Elhalim M.M.
dc.contributor.authorElsayed G.H.
dc.contributor.otherHormones Department
dc.contributor.otherNational Research Centre
dc.contributor.other12622 Dokki
dc.contributor.otherGiza
dc.contributor.otherEgypt; Cell Biology Department
dc.contributor.otherNational Research Centre
dc.contributor.otherDokki
dc.contributor.otherGiza
dc.contributor.otherEgypt; Organic Chemistry Department
dc.contributor.otherFaculty of Pharmacy
dc.contributor.otherOctober University of Modern Sciences and Arts (MSA)
dc.contributor.otherOctober City
dc.contributor.otherEgypt; Chemistry Department
dc.contributor.otherFaculty of Science
dc.contributor.otherCairo University
dc.contributor.otherCario
dc.contributor.otherEgypt
dc.date.accessioned2020-01-25T19:58:29Z
dc.date.available2020-01-25T19:58:29Z
dc.date.issued2011
dc.descriptionScopus
dc.description.abstractAnti-cancer agents which combine two biologically active compounds in one such as steroidal heterocyclic derivatives attain both hormone and cytotoxic effects on cancer cells. The aim of the present study is to synthesize and evaluate new potential chemotherapeutic anti-breast cancer agents. Several pyridazino-, pyrimido-, quinazolo-, oxirano- and thiazolo-steroid derivatives were synthesized. The structure of the novel steroid derivatives was confirmed using the analytical and spectral data. The most structurally promising of the novel synthesized steroid derivatives, compounds 8, 12, 17, 20, 22c, 24c, 30a and 30b, were investigated individually as anti-breast cancer agents against human breast cancer cells (MCF-7) using sulforhodamine B (SRB) assay. The tested compounds 17, 20, 22c and 8 showed potent broad spectrum cytotoxic activity in vitro after 48 h incubation. Compound 17 (IC 50 = 2.5 ?M) exhibited more inhibitory influence on MCF-7 growth than the reference drug doxorubicin (Dox) (IC 50 = 4.5 ?M) after 48 h incubation. Also, the present study showed that all the tested steroid derivatives exhibited significant depletion with various intensities in gene expression of breast cancer related genes (VEGF, CYP19 and hAP-2?). Noteworthy, compounds 17, 20 and 22c showed the most pronounced effect in this respect. � 2011 Elsevier Ltd. All rights reserved.en_US
dc.identifier.doihttps://doi.org/10.1016/j.bmc.2011.09.033
dc.identifier.doiPubMed ID 22000946
dc.identifier.issn9680896
dc.identifier.otherhttps://doi.org/10.1016/j.bmc.2011.09.033
dc.identifier.otherPubMed ID 22000946
dc.identifier.urihttps://t.ly/lW7JL
dc.language.isoEnglishen_US
dc.relation.ispartofseriesBioorganic and Medicinal Chemistry
dc.relation.ispartofseries19
dc.subjectBreast canceren_US
dc.subjectCytotoxicityen_US
dc.subjectGene expressionen_US
dc.subjectHeterocyclesen_US
dc.subjectSteroidsen_US
dc.subject17 [4'(1h) oxo 3' phenyl 2' thioxoquinazolin 1 yl]androst 4 en 3 oneen_US
dc.subject17 chloroandrost 4 en 3 oneen_US
dc.subject2 (3beta acetoxy 5alpha androstan 17 ylideneamino) 4 (methylthio)butanoic aciden_US
dc.subject2 (3beta acetoxy 5alpha androstan 17 ylideneamino) 4 (methythio)butanoic aciden_US
dc.subject2' (3 oxoandrost 4 en 17 yl amino) 5' fluorobenzoic aciden_US
dc.subject2' (3 oxoandrost 4 en 17 yl amino)benzoic aciden_US
dc.subject3' acetylspiro[oxiran 2',17beta 5alpha androstan] 3beta olen_US
dc.subject3' acetylspiro[oxiran 2',3beta andros 4 en] 17beta olen_US
dc.subject3' benzoyl spiro[oxiran 2',17beta 5 alpha androstan] 3beta olen_US
dc.subject3' benzoylspiro[oxiran 2',3beta andros 4 en] 17beta olen_US
dc.subject3' benzoylspiro[oxiran 2',3beta androst 4 en] 17beta olen_US
dc.subject3beta acetoxy 1',3' thiazolo[4',5',:17,16] 5alpha androstan 2' acetonitrileen_US
dc.subject3beta acetoxy 16 bromo 5alpha androstan 17 oneen_US
dc.subject3beta acetoxy 17 ylideneamino(1',4',5',6' tetrahydro 3' hydroxypyridazin 4' yl) 5alpha androstaneen_US
dc.subject3beta acetoxy 17 ylideneamino(n 2' pyrimidylbenzenesulfonamide) 5alpha androstaneen_US
dc.subject3beta acetoxy 17 ylideneamino(n 2' pyrimidylbenzenesulfonamidesodium) 5alpha androstaneen_US
dc.subject3beta acetoxy 17 ylideneamino[2' (n 2inch pyrimidylbenzenesulfonamide)ethanol] 5alpha androstaneen_US
dc.subject3beta acetoxy 2' amino 1',3' thiazolo[4',5':17,16] 5alpha androstaneen_US
dc.subject3beta acetoxy n (diethylenetriamine)copper(II)dinitrite 1',3' thiazolo[4',5':17,16] 5alpha androstaneen_US
dc.subjectantineoplastic agenten_US
dc.subjectaromataseen_US
dc.subjectepidermal growth factor receptoren_US
dc.subjectethyl 17beta hydroxyspiro[oxiran 2',3beta androst 4 en] 3' carboxylateen_US
dc.subjectethyl 3beta hydroxy spiro[oxiran 2',17beta 5alpha androstane] 3 carboxylateen_US
dc.subjectspiro[oxiran 2',17beta 5alpha androstane]en_US
dc.subjectspiro[oxiran 2',3beta 5alpha androstane]en_US
dc.subjectsteroiden_US
dc.subjectsulforhodamine Ben_US
dc.subjectunclassified drugen_US
dc.subjectunindexed drugen_US
dc.subjectvasculotropinen_US
dc.subjectantineoplastic activityen_US
dc.subjectbioassayen_US
dc.subjectbreast canceren_US
dc.subjectcancer cellen_US
dc.subjectconference paperen_US
dc.subjectcontrolled studyen_US
dc.subjectcytotoxicityen_US
dc.subjectdrug potentiationen_US
dc.subjectdrug structureen_US
dc.subjectdrug synthesisen_US
dc.subjectgene expressionen_US
dc.subjectgenetic analysisen_US
dc.subjecthumanen_US
dc.subjecthuman cellen_US
dc.subjectIC 50en_US
dc.subjectin vitro studyen_US
dc.subjectreverse transcription polymerase chain reactionen_US
dc.subjectstructure activity relationen_US
dc.subjectAntineoplastic Agentsen_US
dc.subjectAromataseen_US
dc.subjectBreast Neoplasmsen_US
dc.subjectCell Line, Tumoren_US
dc.subjectDrug Screening Assays, Antitumoren_US
dc.subjectFemaleen_US
dc.subjectGene Expressionen_US
dc.subjectGene Expression Profilingen_US
dc.subjectHumansen_US
dc.subjectInhibitory Concentration 50en_US
dc.subjectSteroidsen_US
dc.subjectStructure-Activity Relationshipen_US
dc.subjectTranscription Factor AP-2en_US
dc.subjectVascular Endothelial Growth Factor Aen_US
dc.titleCytotoxicity and gene expression profiles of novel synthesized steroid derivatives as chemotherapeutic anti-breast cancer agentsen_US
dc.typeConference Paperen_US
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