1186196-63-3

Upstream product

• 45160-42-7 succinic anhydride 
• 108-98-5 thiophenol 
• 103-04-8 (phenylthio)acetic acid 
• 110-15-6 succinic acid 
• 66074-00-8 3,4-bis(phenylsulfonyl)-1,2,5-oxadiazole 2-oxide 
• 108-30-5 succinic acid anhydride 

Downstream Products

• 1309235-26-4 C₃₆H₃₅N₃O₁₀S 
• 1309235-21-9 C₃₂H₃₃N₃O₁₁S 
• 1309235-19-5 C₂₅H₂₇N₃O₁₀S 
• 1309235-18-4 C₃₄H₃₇N₃O₁₂S 
• 1446816-84-7 C₃₄H₃₆N₄O₁₂S 

Relevant academic research and scientific papers

Synthesis of cucurbitacin B derivatives as potential anti-hepatocellular carcinoma agents

Cucurbitacin B shows potent activity against tumor cells, but its high toxicity limits its application in the clinic. A series of cucurbitacin B derivatives was synthesized and evaluated for their anti-hepatocellular carcinoma (HCC) activities against the HepG-2 cell line. These compounds were also tested for their toxicity against the L-O2 normal cell line. The compound with the most potential, 10b, exhibited potent activity against the HepG-2 cell line with an IC50 value of 0.63 μM. Moreover, compound 10b showed the highest TI value (4.71), which is a 14.7-fold improvement compared to its parent compound cucurbitacin B. A preliminary molecular mechanism study of 10b indicated that 10b could inhibit P-STAT3 to induce the activation of mitochondrial apoptotic pathways. An in vivo acute toxicity study indicated that the compound 10b has preferable safety and tolerability compared with cucurbitacin B. These findings indicate that compound 10b might be considered as a lead compound for exploring effective anti-HCC drugs.

Second generation β-elemene nitric oxide derivatives with reasonable linkers: potential hybrids against malignant brain glioma

Elemene is a second-line broad-spectrum anti-tumour drug that has been used in China for more than two decades. However, its main anti-tumour ingredient, β-elemene, has disadvantages, including excessive lipophilicity and relatively weak anti-tumour effic

Discovery of novel antitumor nitric oxide-donating β-elemene hybrids through inhibiting the PI3K/Akt pathway

A series of novel furoxan-based NO-donating β-elemene hybrids were designed and synthesized to improve the anticancer efficacy of natural β-elemene. The bioassay results indicated that all of the target compounds exhibited significantly improved antiproliferative activities against three cancer cell lines (SGC-7901, HeLa and U87) compared to parent compound β-elemene. Interestingly, these compounds displayed excellent sensitivity to U87?cells with IC50 values ranging from 173 to 2?nM. Moreover, most compounds produced high levels of NO in?vitro, and the antitumor activity of 11a in U87?cells was markedly attenuated by an NO scavenger (hemoglobin or carboxy-PTIO). Further mechanism studies revealed that 11a caused the G2 phase arrest of the cell cycle and induced apoptosis of U87?cells by preventing the activation of the PI3K/Akt pathway. Moreover, 11a significantly suppressed the tumor growth in H22 liver cancer xenograft mouse model with a tumor inhibitory ratio (TIR) of 64.8%, which was superior to that of β-elemene (TIR, 49.6%) at the same dose of 60?mg/kg. Together, the remarkable biological profiles of these novel NO-donating β-elemene derivatives may make them promising candidates for the intervention of human cancers.

Nitric oxide-releasing derivatives of brefeldin A as potent and highly selective anticancer agents

A series of NO-donating mono- or diester derivatives of brefeldin A were designed, synthesized and biologically evaluated. Some derivatives exhibited potent antiproliferative activity with low IC50 values. The most potent NO-donating hybrid 13b exhibited stronger cytotoxicity against human prostate cancer PC-3?cells, human colon carcinoma HT-29?cells and human liver cancer HepG-2?cells than BFA with IC50 values of 25?nM, 160?nM and 180?nM, respectively. More importantly, compound 13b showed good selectivity between human normal and tumor liver cells with selectivity index of 33. Additionally, 13b released higher levels of NO in HepG-2?cells than L-02?cells. Further mechanism concerning cellular apoptosis showed that 13b induced apoptosis and S phase cell cycle arrest in HepG-2?cells. Incubation with 13b increased the number of HepG-2?cells with collapsed mitochondrial membrane at low concentrations in dose-dependent manner. In addition, by using the Human Apoptosis Protein Array kit, several apoptosis-related proteins, including HO-1, HO-2 and survivin, were found to be markedly downregulated by 13b in HepG-2?cells. Furthermore, in western blot assay, 13b increased the expression of Bax, Cyt c and caspase 3, and reduced the relative levels of Bcl-2, Bcl-xl and pro-caspase 3 in HepG-2?cells.

Nitric oxide donor type beta-elemene derivative and preparation method and application thereof

The invention belongs to the technical field of the preparation of beta-elemene derivatives, and specifically discloses a nitric oxide donor type beta-elemene derivative and a preparation method and application thereof. The beta-elemene derivative and pha

Gebre Pfund cephalosporin A of 4, 7 - bit double-furazane NO donor substituted derivative and its preparation and use (by machine translation)

The invention relates to the field of pharmaceutical chemistry, relates to the laying of mines Pfund cephalosporin A of 4, 7 - bit at the same time modified derivatives. In particular relates to 4, 7 - bit fufu our kind NO donor substituted BRET Pfund cephalosporin A derivative and its preparation method and in use in the preparation of antineoplastic. The minelaying Pfund cephalosporin A derivatives such as formula I or II is shown, wherein m, n are respectively 1 - 8 of the integer. (by machine translation)

Preparation method and uses of 4-site furazan NO-donating derivatives of brefeldin A

The invention relates to the field of medicinal chemistry, and relates to derivatives obtained by modification on 4-site of brefeldin A. Particularly, the invention relates to 4-site furazan NO donor substituted brefeldin A derivatives which have antineoplastic activity, and uses of the derivatives in preparing antineoplastic drugs. The brefeldin A derivatives are as shown by a general formula I or II, shown in the description, wherein m and n are respectively integers within the range of 1 to 8.

Brefeldin A derivatives, and preparation method and uses thereof

The invention relates to the field of medicinal chemistry, and relates to derivatives obtained by modification on 7-site of brefeldin A. Particularly, the invention relates to 7-site furazan NO donor substituted brefeldin A derivatives, and a preparation method of the derivatives and uses of the derivatives in preparing antineoplastic drugs. The brefeldin A derivatives are as shown by a general formula I or II, shown in the description, wherein m and n are respectively integers within the range of 1 to 8.

Antiproliferative activity and apoptosis inducing effects of nitric oxide donating derivatives of evodiamine

The first series of nitric oxide donating derivatives of evodiamine were designed and prepared. NO releasing ability of all target derivatives was evaluated in BGC-823, Bel-7402 and L-02 cells. The cytotoxicity was evaluated against three human tumor cell lines (Bel-7402, A549 and BGC-823) and normal human liver cells L-02. The nitrate derivatives 11a and 11b only exhibited moderate activity and furoxan-based derivatives 13a-c, 14a and 14b showed promising activity. 13c showed good cytotoxic selectivity between tumor and normal liver cells and was further investigated for its apoptotic properties on human hepatocarcinoma Bel-7402 cells. The molecular mode of action revealed that 13c caused cell-cycle arrest at S phase and induced apoptosis in Bel-7402 cells through mitochondria-related caspase-dependent pathways.

Synthesis, biological activity, and apoptotic properties of NO-donor/enmein-type ent-kauranoid hybrids

Herein, we reported on a series of synthetic nitric oxide-releasing enmein-type diterpenoid hybrids (9a–i). All the target compounds showed potent antibacterial activity against selected Gram-positive bacteria S. aureus and B. subtilis. The antiproliferative activity against human tumor K562, MGC-803, CaEs-17 and Bel-7402 cells, and human normal liver cells L-02 was tested and the structure activity relationships (SARs) were also concluded. Compounds 9b and 9d showed the best activity against S. aureus and B. subtilis with the same minimal inhibitory concentrations (MICs) of 4 and 2 μg/mL, respectively. The derivative 9f displayed IC50 values of 1.68, 1.11, 3.60 and 0.72 μM against the four cancer cell lines above and 18.80 μM against normal liver cells L-02; meanwhile, 9f also released a high level of NO at the time point of 60 min of 22.24 μmol/L. Furthermore, it was also found that 9f induced apoptosis via the mitochondria-related pathway and arrested cell cycle of Bel-7402 cells at S phase. These findings might be important to explore new chemical entities for the main causes of in-hospital mortality of S. aureus infection, combined with a solid tumor.