2. Academic Validation
  3. Synthesis and antitumor activities of 5-methyl-1- and 2-[[2-dimethylaminoethyl]amino]-aza-thiopyranoindazoles

Synthesis and antitumor activities of 5-methyl-1- and 2-[[2-dimethylaminoethyl]amino]-aza-thiopyranoindazoles

  • Bioorg Med Chem Lett. 2000 Feb 7;10(3):305-8. doi: 10.1016/s0960-894x(99)00689-7.
A P Krapcho 1,  S N Haydar,  S Truong-Chiott,  M P Hacker,  E Menta,  G Beggiolin
Affiliations

Affiliation

  • 1 Department of Chemistry, University of Vermont, Burlington 05405, USA. [email protected]
PMID: 10698460 DOI: 10.1016/s0960-894x(99)00689-7
Abstract

The synthesis of 1- and 2-substituted aza-benzothiopyranoindazoles has been accomplished. The comparisons of the in vitro antitumor activities of the 2-substituted analogues with the benzothiopyranoindazole chemotypes indicate that the positioning of the nitrogen atom at C-9 (9-aza analogue 4d) leads to a substrate with potent antitumor activity. The 1-substituted aza-benzothiopyranoindazoles, in comparison with the corresponding 2-substituted analogues, exhibit a much lower potency.

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