Eighteen novel norcantharidin derivatives, which were substituted by chromone ring, were synthesized in a single step by the [3 + 2] 1,3‐dipolar cycloaddition reaction with three oximes in the presence of chloramine‐T when compared with the conventional method.

Canthiridin has significant anti-cancer effects and it is limited to be used due to its toxicity. While cantharidin causes some side effects such as hematochezia and tenesmus, it can efficiently inhibit various tumor cell lines, we must attach importance to it. Several its analogues show similar functions like cantharidin without highly toxicity. In order to utilize cantharidin to treat cancer, some viable methods are found to reduce its side effects. Cantharidin can inhibit the activity of protein phosphatases, new researches for the inhibition of protein phosphatases have been implemented.

Eighteen novel pyrazole‐linked norcantharidin derivatives substituted by chromone ring were synthesized in a single step by the [3+2] 1,3‐dipolar cycloaddition reaction of norcantharidin derivatives of substituted aromatic amines with hydrazone in the presence of chloramine‐T as compared to the conventional method.

It has been a long story of the development of anticancer metallopharmaceuticals since the identification of cisplatin. Advances in metallodrugs discovery during the past 40 years have made it an ever-growing area of research in medicinal inorganic chemistry. Meanwhile, the emerging of N-heterocyclic carbene (NHC) chemistry has stimulated the newly burgeoning interests in the biomedical applications of metal-NHC complexes. This review will detail what have been achieved hitherto in the research of metal-NHC complexes as potential anti-tumor agents coupled with gold, silver, copper, platinum and palladium. Their mechanism of action will also be discussed. All the results obtained indicate that this promising approach is worthy of more focuses and further studies.

Cantharidin (CTD), a natural toxin, can inhibit a variety of tumor cell lines, especially hepatocellular carcinoma cells. It is a strong inhibitor of protein phosphatase type 1 (PP1) and type 2A (PP2A). Because of the cytotoxicity, the clinical application of CDT is limited. Here, we review the structure-activity relationships of CDT analogues, including norcantharidin (NCTD), cantharimides and related derivatives of CTDs, which have more powerful antitumor activity but less cytotoxicity than CDT itself. Important advances in the design of the CTD-based inhibitors achieved recently are outlined here in order to establish principles for synthesis, screening, and the applications of promising anti-cancer drug candidates. In addition, efforts to ameliorate the intrinsic cytotoxicity through the use of drug carriers are also discussed. It is conceivable that rational design of the protein phosphatase inhibitors based on cantharidin analogues can be facilitated by studies of mechanism of the protein-inhibitor interactions and the related structural biology in the future.

Twenty novel norcantharidin derivatives, which were substituted by thiazole ring, were synthesized in a single step by the [3+2] 1,3-dipolar cycloaddition reaction with oxime or hydrazone in the presence of chloramine-T when compared with the conventional method.

We use one molecule of ethylene diamine as a connecting arm to combine two molecules of 5,6-dehydronorcantharidin. Then, ten novel norcantharidin derivatives were synthesized in a single step by the [3 + 2] 1,3-dipolar cycloaddition reaction with oxime or hydrazone in the presence of chloramine-T, which is simpler than the conventional method.

To design and synthesize disodium phosphate of novel norcanthridin analogues. All analogues have been screened for their antiproliferative activity in vitro against a panel of tumour cell lines: SMMC-7721, SGC7901, ECA109, A549 and MCF-7 producing IC50 values from 0.15 mu M to >50 mu M. Compounds 6 and 17 showed potency for the treatment of mammary adenocarcinoma, with IC50 value to MCF-7 cell line comparable to that of cantharidin, which proves that the phosphorylation of norcantharidin analogues is an effective way to increase the activity and solubility.

The asymmetric unit of the racemic title compound, C7H10ClN3O3·0.5H2O, has two independent molecules of ornidazole. The crystal structure is formed via intermolecular hydrogen bonds involving the water molecules.