pyrroloquinoline and Leukemia

pyrroloquinoline has been researched along with Leukemia* in 1 studies

Other Studies

1 other study(ies) available for pyrroloquinoline and Leukemia

Article	Year
Synthesis and in vitro evaluation of 3h-pyrrolo[3,2-f]-quinolin-9-one derivatives that show potent and selective anti-leukemic activity. ChemMedChem, 2010, Aug-02, Volume: 5, Issue:8 A series of new substituted 7-phenyl-3H-pyrrolo[3,2-f]quinolin-9-ones were synthesized and evaluated for their antiproliferative activity. The most active derivatives showed high selectivity against human leukemia cell lines and potently inhibited their growth, with GI(50) values in the nanomolar range. The active compounds strongly blocked tubulin assembly and colchicine binding to tubulin. Their activities were equal to or greater than that of the reference compound combretastatin A-4. Flow cytometry studies showed that the two most active compounds arrested Jurkat cells in the G(2)/M cell-cycle phase in a concentration-dependent manner. This effect was associated with apoptosis, mitochondrial depolarization, generation of reactive oxygen species, activation of caspase-3, and cleavage of the enzyme poly(ADP-ribose) polymerase. Topics: Antineoplastic Agents; Apoptosis; Cell Division; Cell Line, Tumor; Drug Screening Assays, Antitumor; G2 Phase; Humans; Leukemia; Pyrroles; Quinolines; Reactive Oxygen Species; Structure-Activity Relationship; Tubulin; Tubulin Modulators	2010

Article

Year

Synthesis and in vitro evaluation of 3h-pyrrolo[3,2-f]-quinolin-9-one derivatives that show potent and selective anti-leukemic activity.

ChemMedChem, 2010, Aug-02, Volume: 5, Issue:8

A series of new substituted 7-phenyl-3H-pyrrolo[3,2-f]quinolin-9-ones were synthesized and evaluated for their antiproliferative activity. The most active derivatives showed high selectivity against human leukemia cell lines and potently inhibited their growth, with GI(50) values in the nanomolar range. The active compounds strongly blocked tubulin assembly and colchicine binding to tubulin. Their activities were equal to or greater than that of the reference compound combretastatin A-4. Flow cytometry studies showed that the two most active compounds arrested Jurkat cells in the G(2)/M cell-cycle phase in a concentration-dependent manner. This effect was associated with apoptosis, mitochondrial depolarization, generation of reactive oxygen species, activation of caspase-3, and cleavage of the enzyme poly(ADP-ribose) polymerase.

Topics: Antineoplastic Agents; Apoptosis; Cell Division; Cell Line, Tumor; Drug Screening Assays, Antitumor; G2 Phase; Humans; Leukemia; Pyrroles; Quinolines; Reactive Oxygen Species; Structure-Activity Relationship; Tubulin; Tubulin Modulators

2010