Synthesis and Biological Activity of 7-Phenyl-6,9-dihydro-3H-pyrrolo[3,2-f]quinolin-9-ones:  A New Class of Antimitotic Agents Devoid of Aromatase Activity

Abstract

The newly synthesized 7-phenyl-3H-pyrrolo[3,2-f]quinolinones 16-26 and previously 27 and 28 were assayed for their in vitro antiproliferative activity on tumor cell lines, and the lead compound 16 in vivo on a singenic hepatocellular carcinoma in Balb/c mice. Results from FACS, immunofluorescence microscopy analysis, tubulin polymerization assay, and tritiated water release assay for the CYP19 activity confirmed the new compounds as potential anticancer agents acting by tubulin depolymerization, but devoid of aromatase activity unlike their geometric [2,3-h] isomers.

Synthesis, Antimitotic and Antivascular Activity of 1-(3′,4′,5′-Trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles

“…34 Tumors were established by subcutaneous injection of BNL 1ME A.7R.1 cells into the backs of Balb/c mice. In preliminary experiments in vitro, we determined that both compound 3c and CA-4, used as a reference compound, showed similar, potent cytotoxic activity ( 3c IC 50 = 3.4 ± 1.1 nM; CA-4 IC 50 = 1.1 ± 0.5 nM) against BNL 1ME A.7R.1 cells.…”

Multicomponent Reactions in Ionic Liquids

“…Quinolin-4(1H)ones constitute an important class of heterocyclic compounds because of their important pharmaceutical properties, such as anti-viral, [50], [51] anti-platelet, [52] and anti-tumor effects. [53] These compounds have been exploited as precursors for anti-cancer and anti-malarial agents. [54], [ There are many methods for the synthesis of acridine compounds containing 1,4-dihydropyridine moieties from aldehydes, dimedone, and anilines or ammonium acetates via heating in organic solvents, or catalysis by triethyl(benzyl)ammonium chloride (TE-BAC) in water, or under microwave irradiation.…”

Predicting anti-cancer activity of quinoline derivatives: CoMFA and CoMSIA approach

“…Figure 1 shows the display of aligned molecules. Following alignment the molecules were placed within a lattice that extended 4 Å units beyond the aligned molecules in all directions with a grid step size of 2 Å, a probe sp 3 hybridized carbon atom with +1 charge and Van der Waals radius of 1.52 Å was employed.…”

“…[1][2][3] Actinomycin D, doxorubicin, mitoxantrone and streptonigrin are quinoline analogs possessing antibacterial or anti-cancer activity through DNA intercalation. Most of these drugs are currently used in the treatment of human malignancies target topoisomerase (types II) enzymes.…”