Design, synthesis and biological evaluation of novel glyoxalase I inhibitors possessing diazenylbenzenesulfonamide moiety as potential anticancer agents.

Bioorganic & Medicinal Chemistry
Buthina A Al-OudatMel F Bedi

Abstract

The enzyme glyoxalase-I (Glo-I) is an essential therapeutic target in cancer treatment. Significant efforts have been made to discover competitive inhibitors of Glo-I as potential anticancer agents. Herein, we report the synthesis of a series of diazenylbenzenesulfonamide derivatives, their in vitro evaluation against Glo-I and the resulting structure-activity relationships. Among the compounds tested, compounds 9h and 9j exhibited the highest activity with IC50 1.28 µM and 1.13 µM, respectively. Docking studies to explore the binding mode of the compounds identified key moieties that may contribute to the observed activities. The active compounds will serve as suitable leads for further chemical optimization.

References

Jan 1, 1971·Journal of Medicinal Chemistry·R Vince, S Daluge
May 1, 1971·Journal of Medicinal Chemistry·R VinceW B Wadd
Jun 18, 1968·Biochimica Et Biophysica Acta·K NakayaK Shibata
Jun 6, 1969·Biochemical and Biophysical Research Communications·R Vince, W B Wadd
May 23, 2001·Breast Cancer Research and Treatment·A RulliV Talesa
May 31, 2002·Acta Crystallographica. Section D, Biological Crystallography·Helen M BermanChristine Zardecki
Sep 3, 2002·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·E MeariniV N Talesa
Jun 29, 2006·The Cancer Journal·Cinzia AntognelliEttore Mearini
Apr 7, 2007·Cancer Research·George C Prendergast, Elizabeth M Jaffee
May 22, 2007·Bioorganic & Medicinal Chemistry Letters·Swati S More, Robert Vince
Dec 25, 2007·Acta Crystallographica. Section A, Foundations of Crystallography·Helen M Berman
Jan 16, 2008·Protein Engineering, Design & Selection : PEDS·Velin Z SpassovLisa Yan
Aug 21, 2008·Protein Science : a Publication of the Protein Society·Velin Z Spassov, Lisa Yan
Jun 15, 2011·Bioorganic & Medicinal Chemistry Letters·Ryoko TakasawaSei-Ichi Tanuma
Nov 6, 2012·Bioorganic & Medicinal Chemistry Letters·Takashi ChibaHiroshi Koyano
Nov 24, 2012·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Qosay Al-BalasAmmar Almaaytah
Jun 15, 2013·The Biochemical Journal·Marta Sousa SilvaCarlos Cordeiro
Jun 26, 2015·Journal of Biomolecular Structure & Dynamics·Aarti YadavRajat Sandhir
Aug 14, 2015·Current Topics in Medicinal Chemistry·Hong ZhangXiao Peng Hu
Aug 31, 2016·Drug Design, Development and Therapy·Qosay A Al-BalasIsraa H Isawi
Oct 12, 2018·Mini Reviews in Medicinal Chemistry·Qosay A Al-BalasAmmar M Almaaytah
Jan 11, 2019·Journal of Medicinal Chemistry·Christian PerezSeth M Cohen
Apr 5, 2019·Computational Biology and Chemistry·Mahmoud A Al-Sha'erAmmar M Almaaytah

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