Literature DB >> 10021917

Indolocarbazole poisons of human topoisomerase I: regioisomeric analogues of ED-110.

D E Zembower1, H Zhang, J P Lineswala, M J Kuffel, S A Aytes, M M Ames.   

Abstract

All four "symmetrical" regioisomers of ED-110, an indolocarbazole derivative having potent activity against human topoisomerase I (Topo I) were synthesized. The isomer containing hydroxyl groups in the 3- and 9-positions was approximately ten-fold more active against Topo I, and 5- to 35-fold more active against human solid tumor cell lines in vitro, relative to ED-110.

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Year:  1999        PMID： 10021917     DOI： 10.1016/s0960-894x(98)00710-0

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

1.  Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity.

Authors:  Katherine E Peterson; Maris A Cinelli; Andrew E Morrell; Akhil Mehta; Thomas S Dexheimer; Keli Agama; Smitha Antony; Yves Pommier; Mark Cushman
Journal:  J Med Chem       Date:  2011-06-28       Impact factor: 7.446

2.  DNA sequence recognition by the indolocarbazole antitumor antibiotic AT2433-B1 and its diastereoisomer.

Authors:  Carolina Carrasco; Michaël Facompré; John D Chisholm; David L Van Vranken; W David Wilson; Christian Bailly
Journal:  Nucleic Acids Res       Date:  2002-04-15       Impact factor: 16.971

3.  Identification, synthesis, and biological evaluation of metabolites of the experimental cancer treatment drugs indotecan (LMP400) and indimitecan (LMP776) and investigation of isomerically hydroxylated indenoisoquinoline analogues as topoisomerase I poisons.

Authors:  Maris A Cinelli; P V Narasimha Reddy; Peng-Cheng Lv; Jian-Hua Liang; Lian Chen; Keli Agama; Yves Pommier; Richard B van Breemen; Mark Cushman
Journal:  J Med Chem       Date:  2012-12-07       Impact factor: 7.446

4.  Identification of distant drug off-targets by direct superposition of binding pocket surfaces.

Authors:  Marcel Schumann; Roger S Armen
Journal:  PLoS One       Date:  2013-12-31       Impact factor: 3.240

Review 5.  Anomeric modification of carbohydrates using the Mitsunobu reaction.

Authors:  Julia Hain; Patrick Rollin; Werner Klaffke; Thisbe K Lindhorst
Journal:  Beilstein J Org Chem       Date:  2018-06-29       Impact factor: 2.883
  5 in total

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