41102-25-4Relevant academic research and scientific papers
Designing new isomorphic fluorescent nucleobase analogues: the thieno[3,2-d]pyrimidine core
Tor, Yitzhak,Del Valle, Susan,Jaramillo, David,Srivatsan, Seergazhi G.,Rios, Andro,Weizman, Haim
, p. 3608 - 3614 (2007)
A convergent approach for a family of fluorescent nucleosides is described. It relies on thieno[3,2-d]pyrimidine-2,4(1H,3H)-dione that serves as a core heterocycle. This condensed pyrimidine is converted into an emissive pyrimidine nucleoside analogue by N-glycosylation and into an emissive purine nucleoside analogue by C-glycosidation at the thiophene's beta position. The design principles of this archetypical system are outlined together with the syntheses and photophysical properties of the resulting nucleosides.
Identification of Thieno[3,2- d]pyrimidine Derivatives as Dual Inhibitors of Focal Adhesion Kinase and FMS-like Tyrosine Kinase 3
Cho, Hanna,Choi, Hwan Geun,Jeon, Eunhye,Kim, Nam Doo,Kim, Sunghoon,Kim, Younghoon,Kwon, Nam Hoon,Lee, Jiwon,Moon, Youngji,Ryu, Seongshick,Shin, Injae,Sim, Taebo,Song, Chiman,Yoon, Hojong
, p. 11934 - 11957 (2021/08/20)
Focal adhesion kinase (FAK) is overexpressed in highly invasive and metastatic cancers. To identify novel FAK inhibitors, we designed and synthesized various thieno[3,2-d]pyrimidine derivatives. An intensive structure-activity relationship (SAR) study led
COMPOUNDS AS CD73 INHIBITORS
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Paragraph 0162-0163, (2021/05/15)
Provided herein are the compounds that are inhibitors of CD73 and are useful in treating CD73-associated diseases or conditions. Compositions containing the compounds are also provided.
COMPOUNDS FOR TREATING FAMILIAL DYSAUTONOMIA
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Page/Page column 69, (2021/06/22)
The present description relates to compounds useful for improving pre-mRNA splicing in a cell. In particular, another aspect of the present description relates to substituted thieno [3,2-d]pyrimidine compounds, forms, and pharmaceutical compositions there
NOVEL TRYPTOPHAN HYDROXYLASE INHIBITOR AND PHARMACEUTICAL COMPOSITION INCLUDING SAME
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Paragraph 0174; 0177, (2020/07/15)
The present invention relates to a novel tryptophan hydroxylase inhibitor and a pharmaceutical composition including same, wherein the novel tryptophan hydroxylase inhibitor has an excellent inhibitory effect on TPH1, and thus can be usefully used for the prevention or treatment of disorders, such as metabolic disorders, cancer, digestive or cardiovascular system disorders, related to TPH1 activity. In particular, the novel tryptophan hydroxylase inhibitor has an excellent treatment effect on inflammatory bowel disorders, and thus can be usefully used for the treatment of inflammatory bowel disorder.
THIENO- AND PYRROLOPYRIMIDINE ANALOGUES AS ANTICANCER AGENTS AND METHODS OF USE THEREOF
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Paragraph 0066-0067, (2016/09/26)
The present invention provides for the design and synthesis of halogenated thieno- and pyrrolopyrimidine compounds that exhibit cancer proliferation inhibitory activity and the use thereof for cancer treatment.
Antiproliferative activities of halogenated thieno[3,2-d]pyrimidines
Temburnikar, Kartik W.,Zimmermann, Sarah C.,Kim, Nathaniel T.,Ross, Christina R.,Gelbmann, Christopher,Salomon, Christine E.,Wilson, Gerald M.,Balzarini, Jan,Seley-Radtke, Katherine L.
, p. 2113 - 2122 (2014/04/17)
The in vitro evaluation of thieno[3,2-d]pyrimidines identified halogenated compounds 1 and 2 with antiproliferative activity against three different cancer cell lines. A structure activity relationship study indicated the necessity of the chlorine at the C4-position for biological activity. The two most active compounds 1 and 2 were found to induce apoptosis in the leukemia L1210 cell line. Additionally, the compounds were screened against a variety of other microbial targets and as a result, selective activity against several fungi was also observed. The synthesis and preliminary biological results are reported herein.
THIENYL [3,2-D] PYRIMIDIN-4-ONE COMPOUNDS, PREPARATION METHOD, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF
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Paragraph 0120; 0123; 0133; 0136, (2014/11/11)
Disclosed are new thienyl[3,2-d]pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat t
2,4,7-SUBSTITUTED THIENO[3,2-D]PYRIMIDINE COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Paragraph 0135-0137, (2013/03/26)
Disclosed are a 2,4,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel 2,4,7-substituted thieno[3,2-d]pyrimidine compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating diseases caused by abnormal cell growth.
TREATMENT OF CANCERS HAVING K-RAS MUTATIONS
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Paragraph 0616, (2013/05/08)
The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.
