Identification of novel indole based heterocycles as selective estrogen receptor modulator.

dc.contributor.authorSingla, Ramit
dc.contributor.authorPrakash, Kunal
dc.contributor.authorGupta Kunj Bihari
dc.contributor.authorUpadhyay, Shishir
dc.contributor.authorDhiman, Monisha
dc.contributor.authorJaitak, Vikas
dc.date.accessioned2019-03-26T09:01:38Z
dc.date.accessioned2024-08-13T10:34:38Z
dc.date.available2019-03-26T09:01:38Z
dc.date.available2024-08-13T10:34:38Z
dc.date.issued2018
dc.description.abstractIn the present study, we have designed and synthesized indole derivatives by coalescing the indole nucleus with chromene carbonitrile and dihydropyridine nucleus. Two compounds 5c and 6d were selected from series I and II after sequential combinatorial library generation, docking, absorption, distribution, metabolism and excretion (ADME) filtering, anti-proliferative activity, cytotoxicity, and ER-α competitor assay kit by utilizing estrogen receptor-α (ER-α) dominant T47D BC cells line and PBMCs (Peripheral Blood Mononuclear Cells). Cell imaging experiment suggested that both the compounds successfully cross cellular biomembrane and accumulate in nuclear, cytoplasmic and plasma membrane region. Semiquantitative RT-PCR and Western blotting experiments further supported that both compounds reduced the expression of mRNA and receptor protein of ER-α, thereby preventing downstream transactivation and signaling pathway in T47D cells line. Current findings imply that 5cand 6d represent novel ER-α antagonists and may be used in the development of chemotherapy for the management of BC.en_US
dc.identifier.citationSingla, Ramit., Prakash, Kunal., Gupta, Kunj Bihari and et. al. (2018) Identification of novel indole based heterocycles as selective estrogen receptor modulator. Bioorganic Chemistry. Vol. 79, PP. 72-88en_US
dc.identifier.doi10.1016/j.bioorg.2018.04.002
dc.identifier.issn0045-2068
dc.identifier.urihttps://kr.cup.edu.in/handle/32116/2159
dc.identifier.urlhttps://www.sciencedirect.com/science/article/abs/pii/S0045206818302402
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.subjectBreast canceren_US
dc.subjectChromeneen_US
dc.subjectDihydropyridineen_US
dc.subjectEstrogen receptoren_US
dc.subjectIndole derivativesen_US
dc.titleIdentification of novel indole based heterocycles as selective estrogen receptor modulator.en_US
dc.title.journalBioorganic Chemistryen_US
dc.typeArticleen_US
dc.type.accesstypeClosed Accessen_US

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