The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds. ##STR00001##

Disclosed in the present invention is a new triptolide derivative as shown in formula (I). Also disclosed in the present invention are a preparation method for the compound and the medical use thereof in preparation of anti-cancer drugs. Triptolide acrylate of the present invention and a pharmaceutically acceptable salt thereof have anti-cancer activity, and after animal in-vivo experiments, can effectively inhibit tumor growth in animals. A plurality of in-vitro experiments proves that same can significantly increase the protein expression quantity of p53, promote the apoptosis of tumor cells, effectively inhibit the growth of the tumor cells, and have the effect of inhibiting metastasis of cancer cells. More importantly, the toxicity of the compound to normal cells is less than that of triptolide.

##STR00001##

Disclosed in the present invention is a new triptolide derivative as shown in formula (I). Also disclosed in the present invention are a preparation method for the compound and the medical use thereof in preparation of anti-cancer drugs. Triptolide acrylate of the present invention and a pharmaceutically acceptable salt thereof have anti-cancer activity, and after animal in-vivo experiments, can effectively inhibit tumor growth in animals. A plurality of in-vitro experiments proves that same can significantly increase the protein expression quantity of p53, promote the apoptosis of tumor cells, effectively inhibit the growth of the tumor cells, and have the effect of inhibiting metastasis of cancer cells. More importantly, the toxicity of the compound to normal cells is less than that of triptolide.

##STR00001##

Disclosed in the present invention is a new triptolide derivative as shown in formula (I). Also disclosed in the present invention are a preparation method for the compound and the medical use thereof in preparation of anti-cancer drugs. Triptolide acrylate of the present invention and a pharmaceutically acceptable salt thereof have anti-cancer activity, and after animal in-vivo experiments, can effectively inhibit tumor growth in animals. A plurality of in-vitro experiments proves that same can significantly increase the protein expression quantity of p53, promote the apoptosis of tumor cells, effectively inhibit the growth of the tumor cells, and have the effect of inhibiting metastasis of cancer cells. More importantly, the toxicity of the compound to normal cells is less than that of triptolide. ##STR00001##

Disclosed in the present invention is a new triptolide derivative as shown in formula (I). Also disclosed in the present invention are a preparation method for the compound and the medical use thereof in preparation of anti-cancer drugs. Triptolide acrylate of the present invention and a pharmaceutically acceptable salt thereof have anti-cancer activity, and after animal in-vivo experiments, can effectively inhibit tumor growth in animals. A plurality of in-vitro experiments proves that same can significantly increase the protein expression quantity of p53, promote the apoptosis of tumor cells, effectively inhibit the growth of the tumor cells, and have the effect of inhibiting metastasis of cancer cells. More importantly, the toxicity of the compound to normal cells is less than that of triptolide. ##STR00001##

A steroidal piperidone derivative, a synthesis method, and a use thereof are provided. The steroidal piperidone derivative has a chemical structure shown in general formula (1) or general formula (2), where R is any one selected from the group consisting of alkyl, phenyl, substituted phenyl, and a heterocycle. In the synthesis method of the steroidal piperidone derivative, dehydroepiandrosterone (DHEA) is used as a basic raw material to prepare the steroidal piperidone derivative of the present disclosure through a series of reactions. A product prepared by the synthesis method has a high yield and is easily separated, and thus the synthesis method is the optimal method for preparing the steroidal piperidone derivative of the present disclosure. The present steroidal piperidone derivative exhibits prominent toxic activity against sucking pests, such as aphids, spider mites, rice planthoppers, and B. tabaci, and can be used for the control of a plant pest.

##STR00001##

The present invention relates to a combination product comprising a limonoid compound (or a pharmaceutically acceptable derivative, ester, stereoisomer, salt or prodrug thereof), and a biguanide compound (e.g., metformin, metformin hydrochloride, buformin, and phenformin). The present invention further relates to a use of the combination product for prevention and/or treatment of a disease associated with diabetes, for lipid-lowering and weight-loss, and the like.

The present invention relates to a combination product comprising a limonoid compound (or a pharmaceutically acceptable derivative, ester, stereoisomer, salt or prodrug thereof), and a biguanide compound (e.g., metformin, metformin hydrochloride, buformin, and phenformin). The present invention further relates to a use of the combination product for prevention and/or treatment of a disease associated with diabetes, for lipid-lowering and weight-loss, and the like.

N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof.

The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-alkyl- or 2-aromatic-substituted tanshinone I derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments. When Z=R, said derivative is 2-alkyl-substituted tanshinone I; when Z=Ar, said derivative is 2-aryl-substituted tanshinone I; when Z=Het, said derivative is 2-heteroaryl- or 2-heterocyclyl-substituted tanshinone I. ##STR00001##