Literature DB >> 7699706

Rigid analogs of camptothecin as DNA topoisomerase I inhibitors.

K Lackey1, J M Besterman, W Fletcher, P Leitner, B Morton, D D Sternbach.   

Abstract

Substituted 8-ethyl-2-(2-oxo-1,2-dihydroindol-3-ylidene)-8-hydroxy-2,3,5,8- tetrahydro-6-oxa-3a-azacyclopenta[b]naphthalene-1,4,7-triones were synthesized and evaluated as topoisomerase I inhibitors in an in vitro cleavable complex assay. The activity of these compounds may be attributed to their rigid, planar geometry, and an attempt was made to correlate the SAR in this series to known attributes of camptothecin.

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Year:  1995        PMID: 7699706     DOI: 10.1021/jm00006a008

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  2 in total

1.  Comparative molecular field analysis and molecular modeling studies of 20-(S)-camptothecin analogs as inhibitors of DNA topoisomerase I and anticancer/antitumor agents.

Authors:  S W Carrigan; P C Fox; M E Wall; M C Wani; J P Bowen
Journal:  J Comput Aided Mol Des       Date:  1997-01       Impact factor: 3.686

2.  Exploring DNA topoisomerase I ligand space in search of novel anticancer agents.

Authors:  Malgorzata N Drwal; Keli Agama; Laurence P G Wakelin; Yves Pommier; Renate Griffith
Journal:  PLoS One       Date:  2011-09-22       Impact factor: 3.240

  2 in total

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