Tetrahydro-β-carboline-naphthalimide hybrids: Synthesis and anti-proliferative evaluation on estrogen-dependent and triple-negative breast cancer cells

Recent Advances on the Synthesis and Application of Tetrahydro‐β‐Carbolines

“…Recently, a series of tetrahydro‐ β ‐carbolines featuring a naphthalimide moiety linked by diacyl hydrazine were designed and prepared, which were used as potential inhibitors against MCF7 and MDA‐MB‐231 breast cancer cell lines (Scheme 44). [60] SAR studies disclosed that these compounds exhibited almost no inhibitory activities against MDA‐MB‐231 and HEK‐293. However, three tetrahydro‐ β ‐carboline derivatives showed good inhibitory activity against MCF with less than 43 μM IC 50 values.…”

Stereo/regio-selective access to substituted 3-hydroxy-oxindoles with anti-proliferative assessment and in silico validation

“…Our research team recently showed that adding tetrahydro-bcarboline (THbC) to spiro-epoxy oxindoles resulted in 3-THbCsubstituted-3-hydroxy-oxindole with good antiproliferative effects against the MCF-7 (ER+) and MDA-MB-231 (ER) cell lines. 19 Building upon previous studies, [20][21][22] this manuscript focuses on the design, synthesis, characterization, and antiproliferative evaluation of scaffolds that incorporate substituted N-benzylated oxindoles with various secondary amines through nucleophilic ring opening of corresponding oxiranes. To compare the effect of the presence of the N-benzyl group with the free -NH group of the isatin core, the corresponding unsubstituted oxindole counterparts have also been synthesised and evaluated.…”