A novel cyclopalladated ferrocene derivative: Synthesis, single crystal structure and evaluation of in vitro antitumor activity

Publication date: 15 January 2020Source: Journal of Molecular Structure, Volume 1200Author(s): Xingxing Gao, Guidong Gong, Zhonghui Zhang, Guoyuan Du, Yuan Cao, Gang ZhaoAbstractThe cyclopalladated compound (−)-(Sp,R,R,Sp)-3 was obtained by the reaction between acetylferrocene and chiral amines (+)-R-1, followed by palladium acetate and sodium nitrite. (−)-(Sp,R,R,Sp)-3 was characterized by 1H, 13C NMR and ESI-MS. The absolute configuration of the compound (−)-(Sp,R,R,Sp)-3 is determinated by single crystal diffraction. It is found that the compound (−)-(Sp,R,R,Sp)-3 (IC50 = 0.15 μM, 0.49 μM and 0.10 μM) has stronger anticancer activity than the traditional anticancer drug cisplatin (IC50 = 14 μM, 4.6 μM and 4.85 μM) in KGN, HepG2, 4T1 respectively and could be an excellent anticancer drug for treatment of cancer cells.Graphical abstractThe compound (−)-(Sp,R,R,Sp)-3 (IC50 = 0.15 μM) has strong antitumor activity and its IC50 value is 93 times lower than that of cisplatin (IC50 = 14 μM) in KGN.
Source: Journal of Molecular Structure - Category: Molecular Biology Source Type: research