Design, synthesis, and biological evaluation of indole-modified tamoxifen relatives as potent anticancer agents

Abstract

Modulation of existing drugs is an attractive strategy to achieve improved activity in cancer therapy by lowering their effective dose. Preparation of relatives has been suggested and explored to improve...

Development of Novel Pyridine and Pyrimidine Clubbed Bisindoles as Inhibitors of AKT Pathway

“…[4,5] Indole was first synthesized in 1866 by German scientist Adolf von Baeyer, and its derivatives have been studied as potential cancer-inhibiting agents. [6] Several studies have found that certain indole derivatives have anti-cancer effects and may suppress the proliferation of breast cancer cells. [7][8][9] 3,3'diindolylmethane (DIM), which is derived from indole-3-carbinol (I3 C), are found in cruciferous vegetables [10][11][12] has been shown to possess anti-proliferative, pro-apoptotic and anti-angiogenic effects in breast cancer cells by modulating estrogen metabolism, which is relevant in hormone receptor-positive breast cancers.…”

“…Indole was first synthesized in 1866 by German scientist Adolf von Baeyer, and its derivatives have been studied as potential cancer‐inhibiting agents [6] . Several studies have found that certain indole derivatives have anti‐cancer effects and may suppress the proliferation of breast cancer cells [7–9] .…”

“…J = 5.1 Hz, 1H, ArÀ H),6.88 (d, J = 2 4. Hz, 1H, ArÀ H), 6.85 (d, J = 2.4 Hz, 1H, ArÀ H), 6.83 (d, J = 2.3 Hz, 2H, ArÀ H), 6.60 (s, 2H, ArÀ H), 5.74 (s, 1H, ArÀ H), 4.87 (s, 4H, CH2), 1.92 (d, J = 1.3 Hz, 3H, CH 3 ) 2 ); 13 C NMR (400 MHz, CDCl 3 ) δ 154.42, 152.88, 144.32, 143.81, 143.65, 137.73, 137.49, 132.02, 129.39, 129.00, 128.91, 128.51, 128.43, 127.69, 127.52, 127.28, 126.38, 124.41, 122.44, 118.72, 112.66, 111.79, 103.47, 70.80 (CH 2 ), 40.17 (CH), 11.85 (CH 3 ); MS: 643.26, m/z = 643.2638 [M +].…”