The invention discloses a staurosporine compound as well as a preparation method and application thereof. The structure of the compound is of formula I shown in the specification. The compound has antitumor activity and BRD4 inhibition activity, can be used for treating cancer diseases such as leukemia, breast cancer and colon cancer related to over cell proliferation or abnormal cell proliferation, and can be also applied to research and development of medicines related to anti-HIV incubation and anti-human papillomatosis viruses (HPV). According to the preparation method, the staurosporine compound is prepared from marine actinomycete via solid fermentation culture, and a fermentation product is extracted with ethyl acetate and is further separated and purified by using gel chromatography and inversed phase chromatography. The preparation method is easy to operate and implement.

Staurosporine compound as well as preparation method and application thereof

The invention discloses a semisynthetic method of staurosporine derivatives, which comprises the following steps: dissolving raw materials of fermented staurosporine products in a mixed solution of methanol and dichloromethane, adding sodium tungstate dihydrate and an aqueous hydrogen peroxide solution, stirring away from light, adding saturated sodium bisulfite to terminate the reaction, adding hydroxylamine hydrochloride and pyridine, performing extraction, concentration, and recrystallization to obtain a staurosporine derivative 1; dissolving the staurosporine derivative 1 with DMF, adding a TiCl3 aqueous solution, extracting with ethyl acetate for 3 times, washing the organic layer, performing drying by distillation, separation, elution, and crystallization to obtain a staurosporine derivative 2. The invention has cheap and easily available raw materials, and a high yield, and the obtained staurosporine derivatives have important application value in the anti-tumor aspect.

Semisynthetic method of staurosporine derivative

Staurosporine preparation method

The invention discloses an application of a quinazolinone alkaloid compound derived from marine fungi in the prevention and control of marine fouling organisms. The application of the quinazolinone alkaloid compound in the prevention and control of marine fouling organisms is disclosed for the first time, and the quinazolinone alkaloid compound has a significant inhibitory effect on the adhesion of marine fouling organisms on solids, and has a significant effect under low content coating. At the same time, when inhibiting the attachment of marine organisms, it will not kill marine organisms, but will play a repellent role. The compound can not only be extracted from the fermentation products of marine fungi, but also be obtained through artificial mature synthesis process, has reliable andstable sources, and has good application prospects in the prevention and control of fouling organisms in various marine artificial facilities.

Application of Quinazolinone Alkaloid Compound Derived from Marine Fungi in Control of Marine Fouling Organisms

The invention provides a synthesis method for a quinazolinone compound shown as a formula (III). The synthesis method includes adding compounds shown as a formula (I) and a formula (II) into solvents in a reactor; stirring and mixing the compounds and the solvents with one another for 10-15 minutes; then adding catalysts, auxiliaries and accelerators into the reactor; stirring and heating the catalysts, the auxiliaries, the accelerators, the compounds and the solvents until the temperatures of the catalysts, the auxiliaries, the accelerators, the compounds and the solvents reach 60-70 DEG C, carrying out reaction on the catalysts, the auxiliaries, the accelerators, the compounds and the solvents for 8-10 hours to obtain the compound shown as the formula (III). R1 and R2 respectively independently represent alkyl groups or halogen or nitro groups or cyano groups of H, C1, C , C , C , C and C . The synthesis method has the advantages that target products with high yields can be obtained under the mutual synergistic effects of the catalysts, the auxiliaries, the accelerators and the solvents, accordingly, the purpose of developing novel substrate reaction sources for synthesizing the quinazolinone compound can be achieved, and the synthesis method has a broad market prospect.

Synthesis method for quinazolinone compound

The invention relates to quinazoline ketones alkaloid and a preparation method and application thereof; in the invention, separation is carried out in a sea mud sample from offshore Baima Jingzhen in Danzhou in Hainan to obtain bacterium-Baxillus ereus 041381, and the compounds with novel structure are produced by the bacteria with culture preservation number CCTCC M 203030, and the compounds are prepared by a chemical synthesis method; proved by experiments, the compounds have candida albicans resisting activity, the minimum inhibition concentration MIC is 1.3-10.2mum, therefore, the compounds can be used as inhibitors of candida albicans.

Quinazoline ketones alkaloid and preparation method and application thereof

The invention relates to a novel staurosporine analogue and a preparation method and applications thereof, wherein two staurosporine analogue molecules with a novel structure is prepared from the Streptomyces Sp.FMA which is separated from the soil sample of the Sanya Mangrove in Hainan Island of China and has the strain preservation number of CCTCC M 2010021. The in vitro cytotoxicity test proves that the compound has cytotoxicity to leukemia cell HL-60 and lung cancer cell A549 and can be used as the cell antiblastic.

Novel staurosporine analogue and preparation method and applications thereof

The invention relates to cresol trimer compounds as well as a preparation method and application thereof. The compounds with novel structure are prepared from Penicillium expansum 091006 separated from a root sample of Excoecaria agallocha which is a mangrove plant. Proved by experiments, the compounds can be used as a cell proliferation inhibitor or antitumor agent.

Haipeng Lin

Papers

Quinazoline ketones alkaloid and preparation method and application thereof

Novel staurosporine analogue and preparation method and applications thereof

Cresol trimer compounds as well as preparation method and application thereof