A small library of novel copper and zinc imidazo[1,2-a]pyridine complexes have been synthesized. Their structures were confirmed by X-ray diffraction crystallography and a selection of these compounds was tested against five cancer cell lines originating from breast cancer (MCF-7 and MDA-MB-231), leukemia (K562 and HL-60) and colorectal cancer (HT-29). The imidazo[1,2-a]pyridines and their zinc complexes showed poor anticancer activity, while the copper complexes were active against the cancer cell lines with IC₅₀ values comparable to and lower than camptothecin. For example, copper 6-bromo-N-cyclohexyl-2-(pyridin-2-yl)imidazo[1,2-a]pyridin-3-amine acetate 21 had an IC₅₀ value lower than 1 μM against the HT-29 cells. Fluorescence microscopy with acridine orange, Hoechst 33342 and ethidium bromide, used in a preliminary investigation to evaluate morphological changes showed that copper 6-bromo-N-cyclohexyl-2-(pyridin-2-yl)imidazo[1,2-a]pyridin-3-amine acetate 21 caused both apoptosis, necrosis and paraptosis in the MCF-7 and HL-60 cells. A select group of copper N-cyclohexyl-2-(pyridin-2-yl)imidazo[1,2-a]pyridin-3-amines (26, 27, 29 and 31) induced apoptosis, paraptosis and deformed nuclei in MCF-7 cells.

合成了新型铜和锌咪唑并[1,2- a ]吡啶配合物的小型文库。通过X射线衍射晶体学确认了它们的结构，并针对来自乳腺癌（MCF-7和MDA-MB-231），白血病（K562和HL-60）和结直肠癌的五种癌细胞系测试了这些化合物的选择（HT-29）。咪唑并[1,2- a ]吡啶及其锌配合物显示出较差的抗癌活性，而铜配合物对癌细胞系具有活性，其IC ₅₀值与喜树碱相当，且低于喜树碱。例如，铜6-溴-N-环己基-2-（吡啶-2-基）咪唑并[1,2 - a ]吡啶-3-胺乙酸盐21具有IC针对HT-29细胞的₅₀值低于1μM。用a啶橙，Hoechst 33342和溴化乙锭进行的荧光显微镜用于初步研究以评估形态变化，结果表明6-溴-N-环己基-2-（吡啶-2-基）咪唑并[1,2- a ]吡啶铜-3-胺乙酸盐21引起MCF-7和HL-60细胞凋亡，坏死和截瘫。的铜甲选择组ñ -环己基-2-（吡啶-2-基）咪唑并[1,2一]吡啶-3-胺（26，27，29和31）诱导的细胞凋亡，paraptosis和变形核在MCF- 7个单元格。