Department of Chemistry, University of Agriculture Faisalabad-38040, Faisalabad, Pakistan.
School of Chemical Science, Universiti Sains Malaysia, 11800, Penang, Malaysia.
Appl Biochem Biotechnol. 2020 Jul;191(3):1171-1189. doi: 10.1007/s12010-019-03186-9. Epub 2020 Jan 31.
Synthesis and anticancer studies of three symmetrically and non-symmetrically substituted silver(I)-N-Heterocyclic carbene complexes of type [(NHC)-Ag]PF (7-9) and their respective (ligands) benzimidazolium salts (4-6) are described herein. Compound 5 and Ag-NHC-complex 7 were characterized by the single crystal X-ray diffraction technique. Structural studies for 7 showed that the silver(I) center has linear C-Ag-C coordination geometry (180.00(10)). Other azolium and Ag-NHC analogues were confirmed by H and C-NMR spectroscopy. The synthesized analogues were biologically characterized for in vitro anticancer activity against three cancer cell lines including human colorectal cancer (HCT 116), breast cancer (MCF-7), and erythromyeloblastoid leukemia (K-562) cell lines and in terms of in vivo acute oral toxicity (IAOT) in view of agility and body weight of female rats. In vitro anticancer activity showed the values of IC in range 0.31-17.9 μM in case of K-562 and HCT-116 cancer cell lines and 15.1-35.2 μM in case of MCF-7 while taking commercially known anticancer agents 5-fluorouracil, tamoxifen, and betulinic acid which have IC values 5.2, 5.5, and 17.0 μM, respectively. In vivo study revealed vigor and agility of all test animals which explores the biocompatibility and non-toxicity of the test analogues.
本文描述了三种对称和非对称取代的银(I)-N-杂环卡宾配合物[(NHC)-Ag]PF(7-9)及其相应的(配体)苯并咪唑鎓盐(4-6)的合成和抗癌研究。化合物 5 和 Ag-NHC 配合物 7 通过单晶 X 射线衍射技术进行了表征。7 的结构研究表明,银(I)中心具有线性 C-Ag-C 配位几何(180.00(10))。其他唑鎓和 Ag-NHC 类似物通过 H 和 C-NMR 光谱得到证实。合成的类似物在体外对三种癌细胞系(包括人结直肠癌细胞(HCT 116)、乳腺癌细胞(MCF-7)和红白血病母细胞(K-562))进行了抗癌活性测试,并对雌性大鼠的急性口服毒性(IAOT)进行了测试。体外抗癌活性显示,在 K-562 和 HCT-116 癌细胞系中,IC 值范围为 0.31-17.9 μM,在 MCF-7 中为 15.1-35.2 μM,而采用市售抗癌药物 5-氟尿嘧啶、他莫昔芬和白桦酸,其 IC 值分别为 5.2、5.5 和 17.0 μM。体内研究表明,所有试验动物都表现出活力和敏捷性,这证明了试验类似物的生物相容性和非毒性。