Metallodrugs in Medicine

A dual approach to cancer treatment: gold(i) terpyridine derivatives as DNA binders and inhibitors of mammalian thioredoxin reductase

“…Yield 80%. 1 H NMR (400 MHz, d 6 -(CH 3 ) 2 O, ppm): δ 8.71 (m, 2H, H4), 8.60 (m, 2H, H1), 8.45 (d, 2H, H5, 3 J P-H = 7,10 Hz), 7.97 (ddd, 2H, H3, 3 J H3-H2 ∼ 3 J H3-H4 = 7.73 Hz, 4 J H3-H1 = 1.80 Hz), 7.49 (m, 10H, Ph), 7.42 (ddd, 2H, H2, 3 J H2-H3 = 7.50 Hz, 3 J H2-H1 = 4.81 Hz, 4 J H2-H4 = 1.17 Hz). 31 ))] (0.1592 g, 0.32 mmol/0.1724 g, 0.32 mmol) in anhydrous THF (20 mL) is prepared under inert atmosphere, allowing the solution to cool in ice bath for 30 min.…”

“…White solid, yield = 75%. 1 Synthesis of [AuCl(4′-PPh 2 terpy)] (3). To a solution of [AuCl (tht)] (0.1038 g 0.3 mmol) in CH 2 Cl 2 (20 ml) was added 1 equivalent of 4′-PPh 2 terpy (0.1351 g 0.3 mmol).…”

“…Yield 83%. 1 H NMR (400 MHz, d 6 -(CH 3 ) 2 O, ppm): δ 8.74 (m, 2H, H4), 8.66 (d, 2H, H5, J H-P = 13.20 Hz), 8.64 (m, 2H, H1), 8.01 (ddd, 2H, H3, 3 J H3−H2 ∼ 3 J H3-H4 = 7.64 Hz, 4 J H3-H1 = 1.73 Hz), 7.86-7.68 (m, 10H, Ph), 7.48 (ddd, 2H, H2, 3 J H2-H3 = 7.59 Hz, 3 J H2-H1 = 5.92 Hz, 4 J H2-H4 = 1.20 Hz). 31 Synthesis of [Au(CuCR)(4′-PPh 2 terpy)] (R = Ph (4), 2-py (5), CH 2 SPh ( 6)).…”

“…Yellow solid, yield 62%. 1 H NMR (400 MHz, CD 2 Cl 2 , ppm): δ 8.66 (m, 4H, H4 + H1), 8.59 (d, 2H, H5, J H-P = 13.44 Hz), 8.59 (m, 1H, HA) 7.90 (ddd, 2H, H3, 3 J H3-H2 ∼ 3 J H3-H4 = 7.57 Hz, 4 J H3-H1 = 1.74 Hz), 7.76-7.56 (m, 17H, Ph + HD), 7.35 (m, 3H, H2 + HC), 7.71 (m, 1H, HB). 31 P{ 1 H} NMR (162 MHz, CD 2 Cl 2 , ppm) δ 42.24 (s, 1P).…”

Chirality in Anticancer Agents

“…Metal-based antitumor chemotherapeutics obtained prominence after the discovery of the cytotoxic effect of cisplatin -cis-diamminedichloroplatinum (II), cis-[Pt (NH 3 ) 2 Cl 2 ] -Figure 1. Currently, cisplatin is one of the most effective chemotherapeutic drug used for many solid malignancies [16]. The discovery of cisplatin stimulated efforts to investigate other platinum and non platinum metalcontaining compounds for their potential use in the treatment of cancer.…”