Induction of apoptosis and downregulation of ERα in DMBA-induced mammary gland tumors in Sprague–Dawley rats by synthetic 3,5-disubstituted isoxazole derivatives
作者： Hanumappa Ananda , Kothanahally S. Sharath Kumar , Mahesh Hegde , Kanchugarakoppal S. Rangappa
DOI: 10.1007/S11010-016-2777-Z
关键词:
摘要: Isoxazole derivatives are an important group of chemotherapeutic prototypes. In the current study, we have synthesized few isoxazole and tested them for their antiproliferative properties in cancer cell lines such as MCF7 HeLa. The lead compound, 3-(3,4-dimethoxyphenyl)-5-(thiophen-2-yl)isoxazole (2b), showed considerable inhibition proliferation HeLa cells with IC50 values 19.5 39.2 µM, respectively. Cell cycle analyses annexin-FITC staining 2b-treated breast adenocarcinoma (MCF7) increased sub-G1 population apoptosis. Furthermore, tumor inhibitory effect 2b estrogen receptor expression profile DMBA-induced mammary tumors Sprague–Dawley rats. gross morphology studies was investigated by histopathology ERα protein evaluated immunohistochemistry, which regression downregulation cells. present results implicate that compound could be used further derivatization treatment cancer.
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sci-hub.se 参考文章(38)
Apinya Thiantanawat, Angela M. Brodie, Brian J. Long, Signaling pathways of apoptosis activated by aromatase inhibitors and antiestrogens. Cancer Research. ,vol. 63, pp. 8037- 8050 ,(2003)
Mahesh Hegde, Kothanahally S. Sharath Kumar, Elizabeth Thomas, Hanumappa Ananda, Sathees C. Raghavan, Kanchugarakoppal S. Rangappa, A novel benzimidazole derivative binds to the DNA minor groove and induces apoptosis in leukemic cells RSC Advances. ,vol. 5, pp. 93194- 93208 ,(2015) , 10.1039/C5RA16605E
Kothanahally S. Sharath Kumar, Ananda Hanumappa, Maruthai Vetrivel, Mahesh Hegde, Yarabhally R. Girish, Thinnali R. Byregowda, Suguna Rao, Sathees C. Raghavan, Kanchugarakoppal S. Rangappa, Antiproliferative and tumor inhibitory studies of 2,3 disubstituted 4-thiazolidinone derivatives Bioorganic & Medicinal Chemistry Letters. ,vol. 25, pp. 3616- 3620 ,(2015) , 10.1016/J.BMCL.2015.06.069
Irene Barrett, Mary J. Meegan, Rosario B. Hughes, Miriam Carr, Andrew J.S. Knox, Natalia Artemenko, Georgia Golfis, Daniela M. Zisterer, David G. Lloyd, Synthesis, biological evaluation, structural-activity relationship, and docking study for a series of benzoxepin-derived estrogen receptor modulators. Bioorganic & Medicinal Chemistry. ,vol. 16, pp. 9554- 9573 ,(2008) , 10.1016/J.BMC.2008.09.035
Yulia A. Volkova, Elena B. Averina, Yuri K. Grishin, Per Bruheim, Tamara S. Kuznetsova, Nikolai S. Zefirov, Unexpected Heterocyclization of Electrophilic Alkenes by Tetranitromethane in the Presence of Triethylamine. Synthesis of 3-Nitroisoxazoles Journal of Organic Chemistry. ,vol. 84, pp. 3047- 3052 ,(2019) , 10.1021/JO100319P
Stephen Green, Philippe Walter, Vijay Kumar, Andrée Krust, Jean-Marc Bornert, Patrick Argos, Pierre Chambon, Human oestrogen receptor cDNA: sequence, expression and homology to v-erb-A Nature. ,vol. 320, pp. 134- 139 ,(1986) , 10.1038/320134A0
David S. Hewings, Oleg Fedorov, Panagis Filippakopoulos, Sarah Martin, Sarah Picaud, Anthony Tumber, Christopher Wells, Monica M. Olcina, Katherine Freeman, Andrew Gill, Alison J. Ritchie, David W. Sheppard, Angela J. Russell, Ester M. Hammond, Stefan Knapp, Paul E. Brennan, Stuart J. Conway, Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands Journal of Medicinal Chemistry. ,vol. 56, pp. 3217- 3227 ,(2013) , 10.1021/JM301588R
Panagis Filippakopoulos, Stefan Knapp, Targeting bromodomains: epigenetic readers of lysine acetylation Nature Reviews Drug Discovery. ,vol. 13, pp. 337- 356 ,(2014) , 10.1038/NRD4286
Kothanahally S. Sharath Kumar, Ananda Hanumappa, Mahesh Hegde, Kereyagalahally H. Narasimhamurthy, Sathees C. Raghavan, Kanchugarakoppal S. Rangappa, Synthesis and antiproliferative effect of novel 4-thiazolidinone-, pyridine- and piperazine-based conjugates on human leukemic cells European Journal of Medicinal Chemistry. ,vol. 81, pp. 341- 349 ,(2014) , 10.1016/J.EJMECH.2014.05.009
H. Rochefort, J.L. Borgna, E. Evans, Cellular and molecular mechanism of action of antiestrogens Journal of Steroid Biochemistry. ,vol. 19, pp. 69- 74 ,(1983) , 10.1016/S0022-4731(83)80008-9