ISOINDOLO[2,1-C]BENZO[1,2,4]TRIAZINES: A NEW RING SYSTEM WITH ANTIPROLIFERATIVE ACTIVITY

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Abstract

A series of isoindolo-benzo-triazines of type 4 was obtained by diazotization of 2-(2-aminoaryl)-1-cyanoisoindoles 3a–j.All the synthesized derivatives were screened by the National Cancer Institute (NCI, Bethesda, USA), for in vitro antitumor activityagainst a 3-human cancer cell line panel consisting of MCF7 (breast), NCI-H460 (lung), and SF-268 (CNS). Derivatives 4a, f, i, jwere selected to be evaluated in the full panel of about 50 human tumor cell lines derived from nine human cancer cell types andshowed antiproliferative activity generally in the micromolar range. The most sensitive cell lines were: MOLT-4 and SR of the leukemiasubpanel, A549/ATCC and EKVX of the nonsmall cell lung subpanel, COLO-205 of the colon cancer subpanel, LOX IMVIof the Melanoma subpanel, OVCAR-8 of the ovarian cancer subpanel, and MCF7, BT-549 of the breast cancer subpanel.
Lingua originaleEnglish
pagine (da-a)343-349
Numero di pagine7
RivistaBIOORGANIC & MEDICINAL CHEMISTRY
Volume15
Stato di pubblicazionePublished - 2007

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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