Ring fusion strategy for synthesis and lead optimization of sulfur-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-dione derivatives as promising scaffold of antitumor agents

European Journal of Medicinal Chemistry
Yu-Ru LeeHsu-Shan Huang

Abstract

A series of sulfur-substituted anthra[1,2-c][1,2,5]thiadiazole-6,11-diones were synthesized and evaluated using the cell proliferations, apoptosis and NCI-60 cell panel assays. Also, the signaling pathways that account for their activities were investigated. Compounds 2, 3, 4a, 4d, 4f, 4i, 4k, 5b, 5c, 5d, 5f, 5g, 6b, 6c, 6d, 6e, 6g, 7a and 7g were selected by NCI. Among the tested compounds, 6g appeared to be the most active compound of this series that not only induced apoptosis in DU-145 cancer cells but also attenuated the ERK1/2 and p38 signaling pathways. All test compounds exhibited diverse cytostatic and cytotoxic activities that warrant further development as potential anticancer agents.

References

Aug 30, 2001·European Journal of Medicinal Chemistry·C Monneret
Jan 11, 2002·Journal of Medicinal Chemistry·Bernard MasereelClaudiu T Supuran
Nov 7, 2006·IUBMB Life·Zhimin Lu, Shuichan Xu
Jan 24, 2007·Bioorganic & Medicinal Chemistry Letters·Rabindranath TripathyJohn P Mallamo
Aug 10, 2010·European Journal of Medicinal Chemistry·Dalip KumarKavita Shah
Apr 5, 2011·European Journal of Medicinal Chemistry·Malleshappa N NoolviAnkit Chauhan
Aug 23, 2011·The International Journal of Biochemistry & Cell Biology·Yung-Lung ChangShih-Ming Huang
May 15, 2012·The Journal of Antimicrobial Chemotherapy·Fatemeh PourrajabSeyed Ahmad Tabatabaee
Jun 2, 2012·Journal of Enzyme Inhibition and Medicinal Chemistry·Azar TahghighiAlireza Foroumadi
Dec 5, 2012·ChemMedChem·Yijing LiGuisen Zhao
Nov 16, 2013·European Journal of Medicinal Chemistry·Kamal M DawoodPeter Metz
Jan 1, 2013·International Journal of Medicinal Chemistry·Bhawna SharmaUpendra Kumar Sharma
May 20, 2015·Mini Reviews in Medicinal Chemistry·Joanna Matysiak

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Citations

Jul 31, 2019·Medicinal Research Reviews·Xing ChenXin-Hua Liu
Apr 17, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Li-Yun FannSheng-Huang Hsiao
Sep 4, 2020·Pharmacological Reports : PR·Monika Szeliga
Jun 4, 2021·European Journal of Medicinal Chemistry·Yulia L VolodinaAlexander A Shtil
Aug 29, 2021·Medicinal Research Reviews·Kritika LaxmikeshavNagula Shankaraiah

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