Shahsavari Hamid R, Hu Jiyun, Chamyani Samira, Sakamaki Yoshie, Babadi Aghakhanpour Reza, Salmon Christopher, Fereidoonnezhad Masood, Mojaddami Ayyub, Peyvasteh Parnian, Beyzavi Hudson
Department of Chemistry, Institute for Advanced Studies in Basic Sciences (IASBS), Zanjan, 45137-66731, Iran; Department of Chemistry and Biochemistry, University of Arkansas, Fayetteville, Arkansas, 72701, United States.
Department of Chemistry and Biochemistry, University of Arkansas, Fayetteville, Arkansas, 72701, United States.
Organometallics. 2021 Jan 11;40(1):72-82. doi: 10.1021/acs.organomet.0c00728. Epub 2020 Dec 17.
A family of cationic cycloplatinated(II) complexes [Pt(dfppy)(P^P)]Cl, dfppy = 2-(2,4-difluorophenyl)pyridine, incorporating bisphosphine ligands, P^P = bis(diphenylphosphino)methane (, dppm), 1,2-bis(diphenylphosphino)ethane (, dppe) and 1,2-bis(diphenylphosphino)benzene (, dppbz), was prepared. The complexes were characterized by means of several analytical and spectroscopic methods. These complexes displayed acceptable stability in the biological environments which was confirmed by NMR, HR ESI-MS and UV-vis techniques. The antiproliferative properties of these complexes were evaluated by National Cancer Institute (NCI) at National Institutes of Health (NIH) against 60 different human tumor cell lines such as leukemia, melanoma, lung, colon, brain, ovary, breast, prostate and kidney. These complexes showed higher cytotoxicity than cisplatin against a wide variety of cancer cell lines such as K-562 (leukemia), HOP-92 (lung), HCT-116 (colon), OVCAR-8 (ovarian), PC-3 (prostate), MDA-MB-468 (breast), and melanoma cancer cell lines. Complex as the most potent compound in this study furnished an excellent anti-proliferative activity compared to the cisplatin against Hela, SKOV3, and MCF-7 cancer cell lines. The main mode of the interaction of with DNA was also determined using molecular docking studies.
制备了一系列含双膦配体的阳离子环铂（II）配合物[Pt(dfppy)(P^P)]Cl，其中dfppy = 2-(2,4-二氟苯基)吡啶，P^P = 双（二苯基膦基）甲烷（dppm）、1,2-双（二苯基膦基）乙烷（dppe）和1,2-双（二苯基膦基）苯（dppbz）。通过多种分析和光谱方法对这些配合物进行了表征。这些配合物在生物环境中表现出可接受的稳定性，这通过核磁共振、高分辨电喷雾电离质谱和紫外可见光谱技术得到了证实。美国国立卫生研究院（NIH）的美国国立癌症研究所（NCI）评估了这些配合物对60种不同人类肿瘤细胞系（如白血病、黑色素瘤、肺癌、结肠癌、脑癌、卵巢癌、乳腺癌、前列腺癌和肾癌）的抗增殖特性。这些配合物对多种癌细胞系（如K-562（白血病）、HOP-92（肺癌）、HCT-116（结肠癌）、OVCAR-8（卵巢癌）、PC-3（前列腺癌）、MDA-MB-468（乳腺癌）和黑色素瘤癌细胞系）显示出比顺铂更高的细胞毒性。作为本研究中最有效的化合物，配合物 与顺铂相比，对Hela、SKOV3和MCF-7癌细胞系具有出色的抗增殖活性。还通过分子对接研究确定了 与DNA相互作用的主要模式。
