Indoles are natural products which are well known for its anti-cancer activity due to its ability to induce cell death for many cancer cell lines. This review addresses indoles as natural products, mechanism of indoles, facilitated induction and recent studies with indoles and related compounds that were investigated via anti-cancer screening and that led to drug approval.

Arch. Pharm. Pharm. Med. Chem.

No abstract

<p><strong>Objective</strong>:<strong> </strong>The present work aimed to synthesize a new series of 1-methylsulphonyl-3-indolyl heterocycles and study their cytotoxic activity. In addition, we attempted to explore the mode of the interaction of anti-proliferative compounds with the active site of carbonic anhydrase IX (CA IX) theoretically <em>via</em> molecular docking study.</p><p><strong>Methods</strong>:<strong> </strong>Novel series of pyrazole, pyrimidine and triazole derivatives bearing 1-methylsulphonyl-1<em>H</em>-indole were prepared <em>via</em> a series of hetero cyclization reactions utilizing 3-(1-methylsulphonyl-1<em>H</em>-indol-3-yl)-1-(substituted phenyl)-1<em>H</em>-pyrazole-4-carboxaldehydes 3a-d and 3-chloro-3-(1-methylsulphonyl-1<em>H</em>-indol-3-yl)propenal (6) and evaluating their anti-proliferative activity. The structures of the newly synthesized compounds were confirmed by elemental analyses, IR, NMR and mass spectral data. In addition, molecular docking study of the most promising antiproliferative compounds against the active site of carbonic anhydrase IX (PDB ID: 4BCW) theoretically is discussed.</p><p><strong>Results</strong>:<strong> </strong>Compounds 5c, 7 and 12 revealed potent anti-proliferative effects against A-549 cancer cell line with IC₅₀ of 44.3, 17.2 and 38.7 µmol/l, respectively compared to the reference drug doxorubicin (IC₅₀ of 48.8 µmol/l). While compound <strong>5c</strong> was found to be highly active with IC₅₀ of 5.66 µmol/l against HCT-116 cancer cell line than doxorubicin (IC₅₀ of 65.00 µmol/l).</p><p><strong>Conclusion</strong>:<strong> </strong>Further work is recommended to confirm the inhibition of CA IX in a specific bioassay.</p>

A new flavonol glycoside identified as myricetin 3‐O‐β‐D‐sor‐boside (1) has been isolated from the leaves of L. axillare. The new compound showed a moderate inhibition of Ehrlich ascites carci‐noma cells.