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Isoxazole derivatives are an important group of chemotherapeutic prototypes. In the current study, we have synthesized few isoxazole derivatives and tested them for their antiproliferative properties in cancer cell lines such as MCF7 and HeLa. The lead compound, 3-(3,4-dimethoxyphenyl)-5-(thiophen-2-yl)isoxazole (2b), showed considerable inhibition of proliferation of MCF7 and HeLa cells with the IC50 values of 19.5 and 39.2 µM, respectively. Cell cycle analyses and annexin-FITC staining in 2b-treated breast adenocarcinoma cells (MCF7) showed increased sub-G1 population and apoptosis. Furthermore, we tested the tumor inhibitory effect of 2b and estrogen receptor expression profile in DMBA-induced mammary tumors in Sprague-Dawley rats. The gross morphology of tumor studies was investigated by histopathology and ERα protein expression was evaluated by immunohistochemistry, which showed tumor regression and downregulation of ERα in tumor cells. The present results implicate that compound 2b could be used for the further derivatization for the treatment of breast cancer.

Titel:	Induction of apoptosis and downregulation of ERα in DMBA-induced mammary gland tumors in Sprague-Dawley rats by synthetic 3,5-disubstituted isoxazole derivatives.
Autor/in / Beteiligte Person:	Ananda, H ; Kumar, KS ; Hegde, M ; Rangappa, KS
Link:	Full Text Finder (Volltext)
Zeitschrift:	Molecular and cellular biochemistry, Jg. 420 (2016-09-01), Heft 1-2, S. 141-50
Veröffentlichung:	New York : Springer ; <i>Original Publication</i>: The Hague, Dr. W. Junk B. V. Publishers., 2016
Medientyp:	academicJournal
ISSN:	1573-4919 (electronic)
DOI:	10.1007/s11010-016-2777-z
Schlagwort:	Animals Female Humans MCF-7 Cells Rats Rats, Sprague-Dawley 9,10-Dimethyl-1,2-benzanthracene toxicity Androstenols pharmacology Apoptosis drug effects Down-Regulation drug effects Estrogen Receptor alpha biosynthesis Gene Expression Regulation, Neoplastic drug effects Mammary Neoplasms, Experimental chemically induced Mammary Neoplasms, Experimental drug therapy Mammary Neoplasms, Experimental metabolism Mammary Neoplasms, Experimental pathology Neoplasm Proteins biosynthesis
Sonstiges:	Nachgewiesen in: MEDLINE Sprachen: English Publication Type: Journal Article Language: English [Mol Cell Biochem] 2016 Sep; Vol. 420 (1-2), pp. 141-50. <i>Date of Electronic Publication: </i>2016 Jul 29. MeSH Terms: Mammary Neoplasms, Experimental* / chemically induced ; Mammary Neoplasms, Experimental* / drug therapy ; Mammary Neoplasms, Experimental* / metabolism ; Mammary Neoplasms, Experimental* / pathology ; 9,10-Dimethyl-1,2-benzanthracene / toxicity ; Androstenols / pharmacology ; Apoptosis / drug effects ; Down-Regulation / drug effects ; Estrogen Receptor alpha / biosynthesis ; Gene Expression Regulation, Neoplastic / drug effects ; Neoplasm Proteins / *biosynthesis ; Animals ; Female ; Humans ; MCF-7 Cells ; Rats ; Rats, Sprague-Dawley References: J Natl Cancer Inst. 1993 Sep 1;85(17):1412-8. (PMID: 8350365) ; Nat Rev Drug Discov. 2014 May;13(5):337-56. (PMID: 24751816) ; BMC Cancer. 2007 Mar 28;7:56. (PMID: 17391528) ; Cancer Res. 2003 Nov 15;63(22):8037-50. (PMID: 14633737) ; Nat Chem Biol. 2016 Jul;12 (7):504-10. (PMID: 27159579) ; Int J Cancer. 2003 Jul 10;105(5):607-12. (PMID: 12740907) ; N Engl J Med. 2001 Jul 5;345(1):34-40. (PMID: 11439947) ; Proc Natl Acad Sci U S A. 1996 Jun 11;93(12):5925-30. (PMID: 8650195) ; Oncotarget. 2016 Jul 12;7(28):43997-44012. (PMID: 27259267) ; J Carcinog. 2011;10:35. (PMID: 22279420) ; J Med Chem. 2011 Feb 10;54(3):765-81. (PMID: 21204524) ; BMC Cancer. 2009 Apr 08;9:107. (PMID: 19356226) ; Org Biomol Chem. 2011 Nov 7;9(21):7335-42. (PMID: 21887453) ; PLoS One. 2013;8(1):e54055. (PMID: 23342072) ; Nature. 1986 Mar 13-19;320(6058):134-9. (PMID: 3754034) ; J Steroid Biochem. 1983 Jul;19(1A):69-74. (PMID: 6887874) ; Sci Rep. 2015 Sep 21;5:14195. (PMID: 26388336) ; Eur J Med Chem. 2014 Jun 23;81:341-9. (PMID: 24852281) ; J Org Chem. 2010 May 7;75(9):3047-52. (PMID: 20384287) ; Bioorg Med Chem. 2010 May 15;18(10):3437-47. (PMID: 20430632) ; Mol Cell Biol. 2004 Sep;24(17):7681-94. (PMID: 15314175) ; J Med Chem. 2013 Apr 25;56(8):3217-27. (PMID: 23517011) ; Proteins. 2005 May 1;59(2):205-20. (PMID: 15726586) ; Bioorg Med Chem Lett. 2015 Sep 1;25(17):3616-20. (PMID: 26152430) ; Bioorg Med Chem. 2008 Nov 1;16(21):9554-73. (PMID: 18835176) ; Biochem Pharmacol. 2009 Feb 1;77(3):348-63. (PMID: 19014909) ; Int J Mol Med. 2007 Sep;20(3):329-35. (PMID: 17671737) ; J Org Chem. 2013 May 17;78(10):4960-73. (PMID: 23607788) ; BMC Bioinformatics. 2011 Feb 15;12 Suppl 1:S33. (PMID: 21342564) ; Bioorg Med Chem. 2009 May 1;17(9):3479-88. (PMID: 19359182) ; Pharmacol Rev. 2012 Jul;64(3):706-21. (PMID: 22659329) ; J Med Chem. 2011 Oct 13;54(19):6761-70. (PMID: 21851057) ; Pharmacol Rev. 2006 Dec;58(4):773-81. (PMID: 17132854) Contributed Indexing: Keywords: Apoptosis; Cytotoxicity; Dimethylbenzanthracene (DMBA); Estrogen receptor alpha (ERα); Isoxazoles Substance Nomenclature: 0 (Androstenols) ; 0 (Estrogen Receptor alpha) ; 0 (Neoplasm Proteins) ; 1XA84ITL1H (azastene) ; 57-97-6 (9,10-Dimethyl-1,2-benzanthracene) Entry Date(s): Date Created: 20160731 Date Completed: 20170206 Latest Revision: 20181113 Update Code: 20240513

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Induction of apoptosis and downregulation of ERα in DMBA-induced mammary gland tumors in Sprague-Dawley rats by synthetic 3,5-disubstituted isoxazole derivatives.