Department of Chemistry, College of Natural Sciences, Chosun University, 309 Pilmundaero, Gwangju 61452, Republic of Korea.
Molecules. 2023 Jun 23;28(13):4942. doi: 10.3390/molecules28134942.
The objective of this study is to design and synthesize substituted η-chromium(0) tricarbonyl metal complexes carrying -carborane units as potential boron neutron capture therapy (BNCT) agents. In this study, 1,2-diphenyl--carborane () units were used as starting materials to generate biologically active species. We investigated how the structural changes of substituted with chromium(0) tricarbonyl affect the biological properties, and 1-(Phenyl-η-chromium(0) tricarbonyl)-2-phenyl--carborane () and 1,2-bis(phenyl-η-chromium(0) tricarbonyl)--carborane () species were produced in moderate yields. The molecular structures of compounds - were identified and established by infrared (IR); H, B, and C nuclear magnetic resonance (NMR) and X-ray crystallography analyses. Crystal structures of 1,2-diphenyl--carborane and the corresponding chromium complexes , , and were obtained. In an in vitro study using B16 and CT26 cancer cells containing the triphenyl--carboranyl chromium(0) complexes and , which we reported previously, compounds and accumulated at higher levels than compounds and . However, the phenylated -carboranyl chromium complexes have been found to be more cytotoxic than -boronophenylalanine (BPA).
本研究旨在设计和合成取代的η-铬(0)三羰基金属配合物，其带有-卡硼烷单元，作为潜在的硼中子俘获治疗（BNCT）试剂。在本研究中，1,2-二苯基-η-卡硼烷（）单元被用作起始材料，以产生具有生物活性的物质。我们研究了取代铬（0）三羰基的结构变化如何影响生物特性，并且以中等产率生成了 1-(苯基-η-铬(0)三羰基)-2-苯基-η-卡硼烷（）和 1,2-双（苯基-η-铬(0)三羰基）-η-卡硼烷（）。通过红外（IR）；H、B 和 C 核磁共振（NMR）和 X 射线晶体学分析鉴定和确定了化合物 - 的分子结构。获得了 1,2-二苯基-η-卡硼烷和相应的铬配合物、、的晶体结构。在含有我们之前报道的三苯基-η-卡硼基铬(0)配合物和的 B16 和 CT26 癌细胞的体外研究中，与化合物和相比，化合物和在更高水平积累。然而，与硼苯丙氨酸（BPA）相比，苯化-卡硼基铬配合物被发现具有更高的细胞毒性。
