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Literature DB >> 23402879

Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line.

Patricia García-Domínguez¹, Carmela Dell'aversana, Rosana Alvarez, Lucia Altucci, Angel R de Lera.

Abstract

The known DNMT inhibitor SGI-1027 4 has been synthesized using as key steps Pd-catalyzed Ar-N bond formation reactions performed in a sequential or convergent manner. In the former approach, a by-product, which corresponds to the incorporation of two units of 4-chloroquinoline, was also isolated. The biological effects of compound 4 in the U937 human leukemia cell line are also described.

Entities: Chemical Disease Gene Species

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Year: 2013 PMID： 23402879 DOI： 10.1016/j.bmcl.2013.01.085

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

8 in total

1. A rapid screening system evaluates novel inhibitors of DNA methylation and suggests F-box proteins as potential therapeutic targets for high-risk neuroblastoma.

Authors: Livius Penter; Bert Maier; Ute Frede; Benjamin Hackner; Thomas Carell; Christian Hagemeier; Matthias Truss
Journal: Target Oncol Date: 2015-01-06 Impact factor: 4.493

Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line.

1. A rapid screening system evaluates novel inhibitors of DNA methylation and suggests F-box proteins as potential therapeutic targets for high-risk neuroblastoma.

Review 2. Applications of Palladium-Catalyzed C-N Cross-Coupling Reactions.

3. Decitabine enhances stem cell antigen-1 expression in cigarette smoke extract-induced emphysema in animal model.

Review 4. An Epigenetic Role of Mitochondria in Cancer.

5. Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.

6. 5-Aza-2'-deoxycytidine protects against emphysema in mice via suppressing p16^Ink4a expression in lung tissue.

7. DNMTs inhibitor SGI-1027 induces apoptosis in Huh7 human hepatocellular carcinoma cells.

8. 8a, a New Acridine Antiproliferative and Pro-Apoptotic Agent Targeting HDAC1/DNMT1.

Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line.

1. A rapid screening system evaluates novel inhibitors of DNA methylation and suggests F-box proteins as potential therapeutic targets for high-risk neuroblastoma.

Review 2. Applications of Palladium-Catalyzed C-N Cross-Coupling Reactions.

3. Decitabine enhances stem cell antigen-1 expression in cigarette smoke extract-induced emphysema in animal model.

Review 4. An Epigenetic Role of Mitochondria in Cancer.

5. Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer.

6. 5-Aza-2'-deoxycytidine protects against emphysema in mice via suppressing p16Ink4a expression in lung tissue.

7. DNMTs inhibitor SGI-1027 induces apoptosis in Huh7 human hepatocellular carcinoma cells.

8. 8a, a New Acridine Antiproliferative and Pro-Apoptotic Agent Targeting HDAC1/DNMT1.

6. 5-Aza-2'-deoxycytidine protects against emphysema in mice via suppressing p16^Ink4a expression in lung tissue.