5results about How to "Increase structural diversity" patented technology

The invention discloses a tanshinone IIA derivative as well as a preparation method and application thereof, and provides a set of systematic chemical synthesis route for overcoming the defects that tanshinone IIA is poor in water solubility and low in bioavailability and the antitumor activity needs to be improved. A series of novel derivatives with various structures and general formula structures and pharmaceutical salts thereof are prepared. The core of the technical scheme is that after a specific functional group is introduced into the derivative, the water solubility and the stability of the compound are remarkably improved, and the derivative particularly shows excellent anti-colorectal cancer activity, can effectively inhibit tumor cell proliferation and tumor growth in an animal model, and does not have obvious toxic or side effects. The invention also provides a pharmaceutical composition containing the derivative and application of the pharmaceutical composition in preparation of medicines for preventing, relieving or treating colorectal cancer, and provides an important candidate compound for developing a high-efficiency and low-toxicity novel anti-colorectal cancer medicine.

The invention provides an inhibitor for selectively inhibiting cervical cancer C33A cells as well as a preparation method and application of the inhibitor. The invention further provides a preparation method of the novel inhibitor, raw materials are easy to obtain, and the preparation method is simple and feasible. According to the novel inhibitor provided by the invention, the molecular structure diversity of the cervical cancer C33A cell inhibitor is remarkably expanded, and the novel inhibitor can be widely applied to cervical cancer treatment medicines, diagnostic reagents and the like.

The application discloses a terpenoid compound and a preparation method thereof, and belongs to the technical field of biological medicines. A. costaricensis Scale fermentation is carried out, rich secondary metabolites are obtained, and two new terpenoid compounds are obtained through extraction, separation, purification and identification. Compound 1 and compound 2 are both isolated from aspergillus for the first time, so that it is known that under the condition of the culture medium containing halogen salt, the strain can produce secondary metabolites with rich and diverse structures. The application not only enriches the secondary metabolites of aspergillus, expands the structural diversity of aspericin terpenoid compounds, but also preliminarily reveals the anti-tumor activity potential of part of the compounds, so as to lay a material foundation and experimental basis for subsequent in-depth development of activity evaluation, mechanism and structure-activity relationship research.

This application provides a method for the electrocatalytic synthesis of multisubstituted ribose derivatives, comprising using an organotin compound as a catalyst to catalyze the reaction of the compound shown in formula (I) under electrochemical conditions to obtain the compound shown in formula (II); wherein, R 1 C is an optional replacement 1‑10 hydrocarbon group; R 2 and R 3 One of them is -C(=O)OR, and the other is -H; R is the C that can be substituted. 1‑4 Alkyl; R 4 C is a hydrogen atom or an optional substituted C 1‑10 The method involves the use of a hydrocarbon group as the reaction solvent, a reaction temperature of 40-80℃, and a quaternary ammonium bromide as the electrolyte. This method enables the efficient and highly stereoselective synthesis of tetrasubstituted riboses modified with 2'- and 3'-ester groups, and is easily scaled up, showing promising prospects for industrial application. The products obtained by this method possess excellent potential for later derivatization and can be used to synthesize various novel nucleoside analogs, demonstrating significant application value in the development of antiviral and antitumor drugs.

This invention discloses a method and system for expanding underwater image datasets based on a generative model. The method first constructs a pairing dataset of side-scan sonar images and text descriptions. After encoding the images into the latent space and adding noise, the LoRA module is used for fine-tuning while freezing the parameters of the basic diffusion model, enabling the model to learn the bright areas, shadow areas, and background texture features in the side-scan sonar images. Subsequently, new samples are generated based on preset prompts, and these generated samples are filtered and fused with the original samples to form an expanded dataset. This approach can improve the structural diversity and style consistency of side-scan sonar training samples, reduce data acquisition and annotation costs, and improve the training effect of downstream target detection models.