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2000
Volume 18, Issue 10
  • ISSN: 1386-2073
  • E-ISSN: 1875-5402

Abstract

A series of benzo[a]pyrano[2,3-c]phenazine derivatives with a wide range of substitutions at ring C of the benzophenazine were designed and synthesized using the one-pot, four-component domino reactions. The targeted compounds were evaluated for their antitumor activities against HCT116, MCF7, HepG2 and A549 cancer cell lines in vitro. The most active compound 6{1,2,1,9} featured the CN and p-dimethylamino phenyl substituents on γ-pyran structure on ring C. Significantly, compound 6{1,2,1,9} was found to have the highest growth inhibitory activity against the HepG2 cell line with IC50 values of 6.71 µM, which was 1.6-fold more potent than positive control anticancer drug Hydroxycamptothecine (HCPT). Furthermore, structure-activity relationship (SAR) studies on the substitutions at ring C were discussed in details.

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/content/journals/cchts/10.2174/1386207318666150915113549
2015-12-01
2025-07-12
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  • Article Type:
    Research Article
Keyword(s): 3-c]phenazine; Antitumor activity; benzo[a]pyrano[2; SAR
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