Synthesis and Cytotoxic Properties of 3,4-dihydro-3-oxo-2H-1,2,4-benzothiadiazine-1,1-dioxides

3,4-디히드로-3-옥소-2H-1,2,4-벤조치아디아진-1,1-디옥사이드 유도체의 합성 및 세포 독성

  • 박혜영 (이화여자대학교 약학대학) ;
  • 한윤정 (이화여자대학교 약학대학) ;
  • 이정옥 (한국화학연구소 의약활성센터)
  • Published : 1995.12.01

Abstract

A series of 3, 4-dihydro-3-oxo-2H-1, 2, 4-benzothiadiazine-1, 1, dioxides with cytotoxic activity against human solid tumors is described. Synthesized compounds showed mild but broad spectrum cytotoxicity in vitro. The lipophilic substituents like alkyl, alkoxy and chloro on benzene ring increased the activity. Also hydrophobic group on 3 or 4 position of benzothiadiazine was important for the activity.

Keywords

References

  1. Proc. Am. Assoc. Cancer Res. v.535 Identification of diarylsulfonylureas as novel anticancer drugs Grindey,G.B.
  2. Cancer Cells v.2 Currunt status of cancer drug development : faliure or limited success? Grindey,G.B.
  3. Cancer Res. v.51 Effect of antitumor diarylsulfonylureas on in vivo and in vitro mitochondrial structure and functions Thakar,J.H.;Chapin,C.;Houghton,P.J.
  4. Drug Metab. dispos v.19 Metabolism and disposition of the anticancer agent sulofenur in mouse, rat, monkey and human William,J.E.
  5. Drug of the future v.16 Sulofenur Howbert,J.J.
  6. J. Med. Chem. v.33 Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure activity relationships Grossman,C.S.;Howbert,J.J.;Crowell,T.A.;Rieder,B.J.;Harper,R.W.;Kramer,K.E.;Tao,E.V.;Aikins,J.;Poore,J.A.;Rinzel,S.M.;Grindey,G.B.;Shaw,W.H.;Todd,G.C.
  7. Drug of the future v.17 Discovery of novel antineoplastic sulfonylureas Border,B.B.;Ehlhardt,W.J.;Grindey,G.B.;Houghton,P.J.
  8. J. Chem. Soc. Perkin Trans v.1 A new synthesis of 1,2,4-benzothiadiazines and a selective preparation of o-aminobenzenesulfonamides Yves,G.;Atkinson,J.
  9. J. Med. Chem. v.33 Synthesis and biological evaluation of 2-styrylquinazolin-4(3H)-ones, a new class of antimitotoxic anticancer agents which inhibit tibilin polymerization Jiang,J.B.;Hessen,D.D.;Dusak,B.A.;Dexter,D.L.;Kang,G.J.;Hamel,E.
  10. J. Natl. Cancer Inst. v.83 Feasibility of a high-flux anticancer drug screen using a diverse panel of cultured human tumor cell lines Monks,A.;Scudiero,D.;Srehan,P.;Shoemaker,R.;Kenneth,P.;David,V.;Hose,C.;Langley,J.;Cronise,P.