Cancer is the abnormal division and multiplication of cells in an organ or tissue. It is the second leading cause of death globally. There are various types of cancer such as prostate, breast, colon, lung, stomach, liver, skin, and many others depending on the tissue or organ where the abnormal growth originates. Despite the huge investment in the development of anticancer agents, the transition of research to medications that improve substantially the treatment of cancer is less than 10%. Cisplatin and its analogs are ubiquitous metal-based anticancer agents notable for the treatment of various cancerous cells and tumors but unfortunately accompanied by large toxicities due to low selectivity between cancerous and normal cells. The improved toxicity profile of cisplatin analogs bearing bidentate ligands has motivated the synthesis of vast metal complexes of bidentate ligands. Complexes derived from bidentate ligands such as β-diketones, diolefins, benzimidazoles and dithiocarbamates have been reported to possess 20 to 15,600-fold better anticancer activity, when tested on cell lines, than some known antitumor drugs currently on the market, e.g. cisplatin, oxaliplatin, carboplatin, doxorubicin, and 5-fluorouracil. This work discusses the anticancer properties of various metal complexes derived from bidentate ligands, for possible application in chemotherapy. The results discussed were evaluated by the IC₅₀ values as obtained from cell line tests on various metal-bidentate complexes. The structure-activity relationship study of the complexes discussed, revealed that hydrophobicity is a key factor that influences anticancer properties of molecules.

癌症是器官或组织中细胞的异常分裂和增殖。它是全球第二大死亡原因。癌症有多种类型，如前列腺癌、乳腺癌、结肠癌、肺癌、胃癌、肝癌、皮肤癌等，具体取决于异常生长的组织或器官。尽管在抗癌药物的开发上投入了巨额资金，但研究转向显着改善癌症治疗的药物的比例还不到 10%。顺铂及其类似物是普遍存在的金属基抗癌剂，以治疗各种癌细胞和肿瘤而闻名，但不幸的是，由于癌细胞和正常细胞之间的选择性较低，因此伴随着较大的毒性。带有二齿配体的顺铂类似物的毒性特征的改善促进了二齿配体的大量金属配合物的合成。据报道，在细胞系上测试时，源自双齿配体（例如 β-二酮、二烯烃、苯并咪唑和二硫代氨基甲酸盐）的复合物具有比目前市场上一些已知的抗肿瘤药物（例如顺铂、奥沙利铂）高 20 至 15,600 倍的抗癌活性、卡铂、阿霉素和5-氟尿嘧啶。这项工作讨论了衍生自双齿配体的各种金属配合物的抗癌特性，以及在化疗中的可能应用。所讨论的结果通过从各种金属-二齿络合物的细胞系测试中获得的IC ₅₀值来评估。对所讨论的配合物的构效关系研究表明，疏水性是影响分子抗癌特性的关键因素。