1245575-37-4

Upstream product

• 77279-24-4 tert-butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate 
• 66074-00-8 3,4-bis(phenylsulfonyl)-1,2,5-oxadiazole 2-oxide 
• 103-76-4 1-(2-hydroxyethyl)piperazine 

Downstream Products

• 1245575-23-8 3-(phenylsulfonyl)-4-(2-(4-(2-((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienylthio)benzoyl)piperazin-1-yl)ethoxy)-1,2,5-oxadiazole-2-oxide 
• 1588522-96-6 4-(2-(4-(3-((3-((5-chloro-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)amino)-3-oxopropyl)piperazin-1-yl)ethoxy)-3-(phenylsulfonyl)-1,2,5-oxadiazole 2-oxide 
• 1436851-33-0 C₄₀H₄₃ClN₁₀O₉S 

Relevant academic research and scientific papers

Chromone 3-piperazine linked furazan derivative as well as preparation method and application thereof

The invention relates to the fields of natural medicines and medicinal chemistry, and relates to a preparation method of a series of chromone 3-piperazine linked furazan derivatives with antitumor activity and a new application of the chromone 3-piperazine linked furazan derivatives in preparation of antitumor medicines. The chromone 3-piperazine linked furazan derivative and the pharmaceutically acceptable salt thereof disclosed by the invention are as shown in a general formula I in the specification. Wherein R is described in the claims and the specification.

Chromone 2-piperazine linked furazan derivative as well as preparation method and application thereof

The invention relates to the fields of natural medicines and medicinal chemistry, and relates to a preparation method of a series of chromone 2-piperazine linked furazan derivatives with antitumor activity and a new application of the chromone 2-piperazine linked furazan derivatives in preparation of antitumor medicines. The chromone 2-piperazine linked furazan derivative and the pharmaceutically acceptable salt thereof disclosed by the invention are as shown in a general formula I in the specification. Wherein R is described in the claims and the specification.

Discovery of β-carboline-(phenylsulfonyl)furoxan hybrids as potential anti-breast cancer agents

The cytotoxicity properties of the β-carboline alkaloids have been broadly investigated. However, the potential application of β-carbolines was hindered due to the moderate activity in cancer. In the present study, thirty β-carboline-(phenylsulfonyl)furoxan hybrids (11a–j, 12a–j and 13a–j) were designed and synthesized through esterification and amidation reaction strategy, and their inhibitory activities against the human breast cancer cell lines MCF-7 and MDA-MB-231 were evaluated by CCK-8 assay. Biological evaluation presented that the most promising amide derivative 13h, substituted with p-methoxyphenyl group at position 1, generated high concentration of NO and evidently depressed the MCF-7 (IC50 = 0.89 μM) and MDA-MB-231 (IC50 = 0.62 μM) cells proliferation. Particularly, the wound healing and transwell assays demonstrated that 13h significantly inhibited the migration and invasion of MDA-MB-231cells. Furthermore, the preliminary mechanisms studies indicated that 13h induced G2/M phase arrest and apoptosis possibly causing by ROS accumulation and ROS-mediated DNA damage. Based on these considerations, 13h may be a promising antimetastatic agent for breast cancer, which is noteworthy for further exploration.

Nitric oxide-donating and reactive oxygen species-responsive prochelators based on 8-hydroxyquinoline as anticancer agents

Metal ion chelators based on 8-hydroxyquinoline (8-HQ) have been widely explored for the treatment of many diseases. When aimed at being developed into potent anticancer agent, a largely unmet issue is how to avoid nonspecific chelation of metal ions by 8

Antiproliferative chromone derivatives induce K562 cell death through endogenous and exogenous pathways

A series of furoxan derivatives of chromone were prepared. The antiproliferative activities were tested against five cancer cell lines HepG2, MCF-7, HCT-116, B16, and K562, and two normal human cell lines L-02 and PBMCs. Among them, compound 15a exhibited the most potent antiproliferative activity. It was also found 15a produced more than 8 μM of NO at the peak time of 45 min by Griess assay. Generally, antiproliferative activity is positively related to NO release to some extent. Further in-depth studies on apoptosis-related mechanisms showed that 15a caused S-phase cell cycle arrest in a concentration-dependent manner and induced apoptosis significantly through mitochondria-related pathways. Human apoptosis protein array assay also demonstrated 15a increased the expression levels of pro-apoptotic Bax, Bad, HtrA2 and Trail R2/DR5. The expression of catalase and cell cycle blocker claspin were similarly up-regulated. In balance, 15a induced K562 cells death through both endogenous and exogenous pathways.

NO donor compounds, compositions, preparation method and application thereof

The object of the present invention is to provide NO donor compounds, compositions, a preparation method and application thereof. The compounds and the compositions show high anticancer activity in in-vitro anticancer activity tests, and have inhibitory a

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.

Scutellarin derivatives as apoptosis inducers: Design, synthesis and biological evaluation

To explore novel antitumor agents with high efficiency and low toxicity, a series of NO-donating scutellarin derivatives (14–17) were synthesized and the antiproliferative activities against MCF-7, HCT-116, PC-3 and HepG2 cancer cell lines were assessed. Among them, compound 14b was the strongest with IC50 values of 2.96?μM, 7.25?μM, 0.09?μM and 0.50?μM, respectively, and displayed low toxicity against normal human liver L-O2 cells with an IC50 of 47.96?μM, showing good selectivity between normal and malignant liver cells. Moreover, NO releasing ability of the derivatives has been studied. Mechanism studies of the most promising compounds 14b and 15a were carried out. The results indicated that 14b and 15a could induce apoptosis, cell cycle arrest at the S phase and led to mitochondrial dysfunction in the HepG2 and PC-3?cell lines, respectively. Furthermore, Human Apoptosis Protein Array kit assay demonstrated that 14b could induce apoptosis through down-regulating the levels of procaspase-3 and inhibiting the expression of survivin, c-IAP1, HSP27, HSP60, HSP70, HO-1/HMOX1/HSP32 and HO-2/HMOX2 in HepG2 cell line. These results guaranteed compound 14b to be a drug candidate against liver cancer for further investigation.

Furazan type NO (nitric oxide) donor scutellarin derivative with anti-tumor activity and preparation method and application thereof

The invention relates to the field of natural medicines and medicine chemistry, in particular to a furazan type NO (nitric oxide) donor scutellarin derivative with anti-tumor activity and a pharmaceutically acceptable salt thereof, and in particular to a furazan type NO donor-substituted scutellarin derivative with a piperazine ringfatty chain link arm on saccharide carboxyl sites and a preparation method and application thereof in preparing anti-tumor medicines. The structures of the furazan type NO donor scutellarin derivative with anti-tumor activity and the pharmaceutically acceptable salt thereof are shown in the formula I, wherein R and n R1 are described in the right claim and instructiondescription. The formula I is shown in the descriptionattached figure.

Design, synthesis and evaluation of nitric oxide-releasing derivatives of N-(n-butyl)matrinic acid and N-(n-butyl)matrinol as anti-hepatocellular carcinoma agents

A series of novel furoxan-based derivatives of N-n-butyl matrinic acid (9a-m) and N-n-butyl matrinol (10a-m) were synthesized and their anti-human hepatocellular carcinoma (HCC) activities were evaluated. All derivatives displayed potential inhibition of