Multicomponent assembly of 4-aza-podophyllotoxins: A fast entry to highly selective and potent anti-leukemic agents

Synthesis and biological activity, and molecular modelling studies of potent cytotoxic podophyllotoxin-naphthoquinone compounds

“…4,5 Moreover, podophyllotoxin derivatives possess cathartic, antirheumatic, antiviral and antitumor properties. [6][7][8] Among podophyllotoxin analogues, 4-aza-podophyllotoxins have attracted considerable attention in anticancer drug discovery, [9][10][11][12][13][14] owing to their important biological activities in cell cycle arrest in the G2/M phase, 15,16 and caspase-3 dependent apoptosis, 17 and as tubulin assembly inhibitors, 17 vasculardisrupting agents, 18 antitumor agents, 19 and insecticides (larvicidal). 20 The g-butyrolactone ring D of 4-azapodophyllotoxins has played a vital role in the biological activities through binding to tubulin, 21 and its modications caused a decrease of cytotoxicity in the derivatives.…”

“…7,[21][22][23] The 3,4,5-trimethoxy substitutions of the E-ring generally resulted in an improvement in cytotoxicity. 9 On the other hand, the nitrogen heterocyclic compounds have attracted the interest of scientists due to their bioactive properties. [24][25][26][27][28][29][30][31][32] Aza-anthraquinones, which are crucial analogues of 1,4naphthoquinones, have known as intercalating DNA binding agents in cancer chemotherapy due to the planar structure (Fig.…”

“…7,21–23 The 3,4,5-trimethoxy substitutions of the E-ring generally resulted in an improvement in cytotoxicity. 9…”

Quinoline-Fused Lactones via Tandem Oxidation Cyclization: Metal-Free sp3 C–H Functionalization

“…1,4-Dihydroquinoline lactones ( I ), derived by reduction of 9-phenylfuro­[3,4- b ]­quinolin-1­(3 H )-one, are known for their anti-leishmanial and anti-leukemic properties. Another biologically important molecule, 3-fluoromethylquinoline-2-carboxamide ([ 18 F]-AB5186) ( II ), known as a positron emission tomography imaging agent can be derived from 9-phenylfuro­[3,4- b ]­quinolin-1­(3 H )-one …”

The efficient in‐situ reduction and cyclization reaction of aromatic aldehyde, 1,3‐cyclopentanedione (tetronic acid), and nitro‐compound under SnCl2·2H2O‐THF medium

“…As reported literatures, anilines, aldehyde and ketones were often used for the synthesis of nitrogen‐containing heterocyclic compounds . Recently, pyrazolo[4,3‐ f ]quinoline, pyrazolo[3,4‐ f ]quinoline derivatives were also effectively obtained from amino compounds, such as 5‐aminoindazole, 6‐aminoindazole, 5‐amine‐1 H ‐indole, and so on .…”