920744-71-4

Upstream product

• 583-52-8 potassium oxalate 
• 108-91-8 cyclohexylamine 
• 209861-57-4 C₆H₂₀N₂O₂Pt⁽²⁺⁾ 
• 146924-19-8 cis-Pt(NH₃)(cyclohexylamine)I₂ 
• 62-76-0 sodium oxalate 

Relevant academic research and scientific papers

Synthesis, characterization, and antitumor activity of novel tumor-targeted platinum(IV) complexes

Four tumor-targeted platinum(IV) complexes with ammonia and cyclohexylamine as the carrier groups and biotin as the axial group were designed, synthesized, and characterized. In vitro evaluation of the antitumor activity of complexes C1–C4 against lung cancer cells (A549), liver cancer cells (SMMC-7721), breast cancer cells (MCF-7), and colon cancer cells (SW480) was carried out. Complex C3 had the best cellular activity. Compared with cisplatin, complex C3 showed good anticancer activity against A549 cell line,complex C3 (6.34±0.44) is 3 times more cytotoxic than cisplatin (19.40±0.71),and against MCF-7 cell line complex C3 (4.22±0.11) is 5.4 times more cytotoxic than cisplatin (22.96±0.58), and against SW480 cell line complex C3 (6.65±0.60) is 3.4 times more cytotoxic than cisplatin (23.15±0.22). (Table 1) Axial chloride increased the redox power of complex C3 to increase the intercellular accumulation and the introduction of mixed amine had the ability to overcome cisplatin resistance. Complex C3 works best on MCF-7, then SW480, A549, and SMMC-7721. Thus, complex C3 is targeted by the axial introduction of biotin.

Preparation method and application of novel Pt(IV) complex with tumor targeting function

The invention discloses a novel Pt(IV) complex with a tumor targeting function. The complex has a structure represented by the formula (I) or the formula (II). The invention discloses a preparation method of the novel Pt(IV) complex. According to the preparation method, an asymmetric ammonia ligand of a Satraplatin carrier group is maintained, a biotin ligand with a targeting function is introduced into one axial end, chloride is introduced into the other end so as to reduce the negative value of the redox potential of the platinum complex, the reducing power is increased at the same time; ora hydroxyl group of the other end is maintained, thus after the Pt(IV) complex enters a human body, the Pt(IV) complex can preferably combine with a reducing agent in the human body, and the Pt(IV) complex is reduced to obtain Pt(II) complex so as to treat the tumors. The provided Pt(IV) complex has antitumor activity on specific tumors, and the toxic effect and side effect are reduced. At the same time, the raw materials are cheap and easily available, the preparation method is simple and is easy to perform, the conditions are mild, the operation is easy, and the preparation method is suitable for large scale production. Z is Cl.

Synthesis, cytotoxicity, and DNA-binding levels of ammine/cyclohexylamine platinum(II) complexes with dicarboxylates

Four new ammine/cyclohexylamine platinum(II) complexes with dicarboxylates (a-d) have been synthesized and characterized by elemental analysis, conductivity, IR, UV, and 1HNMR spectra techniques. The cytotoxicity of the complexes was tested by MTT assay. The cell cycle analysis and the levels of total platinum bound to DNA were measured by flow cytometry and ICP-MS. The results show that the cytotoxicity of complexes (a-d) against EJ, HCT-8, BGC-823, HL-60, and MCF-7 cell lines decreases in the sequence: b > a > c > d. Complexes (a-d) have better cytotoxicity against EJ and HL-60 and complex (b) demonstrates cytotoxicity superior to that of the clinically established cisplatin. The complexes (a-d) induced a concentration-dependent accumulation of HL-60 cells in the G2/M phase of the cell cycle as cisplatin. The levels of total platinum bound to DNA in HL-60 and EJ cells decrease in the sequence: b > cisplatin > a > c > d under the same experimental conditions. Copyright