63894-67-7

Usage

Uses

Used in Pharmaceutical Industry:
4-(2-chlorothieno[2,3-d]pyrimidin-4-yl)Morpholine is used as a pharmaceutical intermediate for the synthesis of various drugs and chemical compounds. Its unique structure allows it to be a key component in the creation of new medications, contributing to the advancement of pharmaceutical research and development.
Used in Drug Development:
In the realm of drug development, 4-(2-chlorothieno[2,3-d]pyrimidin-4-yl)Morpholine is utilized as a building block for designing and synthesizing novel therapeutic agents. Its incorporation into drug molecules can potentially enhance their efficacy, selectivity, and pharmacokinetic properties, thereby improving treatment outcomes for patients.
Used in Medicinal Chemistry Research:
4-(2-chlorothieno[2,3-d]pyrimidin-4-yl)Morpholine is also used in medicinal chemistry research to explore its chemical properties, reactivity, and potential interactions with biological targets. This research is vital for understanding the compound's behavior and optimizing its use in drug discovery processes.
Safety Considerations:
Due to its potential hazards and reactivity, it is essential to handle 4-(2-chlorothieno[2,3-d]pyrimidin-4-yl)Morpholine with caution and adhere to proper safety protocols. Further research and testing may be necessary to fully comprehend its properties and potential applications, ensuring its safe and effective use in pharmaceutical formulations.

Upstream product

• 18740-38-0 1H-thieno[2,3-d]pyrimidine-2,4-dione 
• 4651-81-4 Methyl 2-aminothiophene-3-carboxylate 
• 110-91-8 morpholine 
• 18740-39-1 2,4-dichlorothieno[2,3-d]pyrimidine 

Downstream Products

• 1033744-45-4 4-(2-chloro-6-(3-(methylsulfonyl)phenyl)thieno[2,3-d ]pyrimidin-4-yl)morpholine 
• 1033735-40-8 5-(6-(3-(methylsulfonyl)phenyl)-4-morpholinothieno[2,3-d]-pyrimidin-2-yl)pyrimidin-2-amine 

Relevant academic research and scientific papers

Design, synthesis, and biological evaluation of novel thienopyrimidine derivatives as PI3Kα inhibitors

Three series of novel thienopyrimidine derivatives 9a-l, 15a-l, and 18a-h were designed and synthesized, and their IC50 values against four cancer cell lines HepG-2, A549, PC-3, and MCF-7 were evaluated. Most compounds show moderate cytotoxicity against the tested cancer cell lines. The most promising compound 9a showed moderate activity with IC50 values of 12.32 ± 0.96, 11.30 ± 1.19, 14.69 ± 1.32, and 9.80 ± 0.93 μM, respectively. The inhibitory activities of compounds 9a and 15a against PI3Kα and mTOR kinase were further evaluated. Compound 9a exhibited PI3Kα kinase inhibitory activity with IC50 of 9.47 ± 0.63 μM. In addition, docking studies of compounds 9a and 15a were also investigated.

COMPOUNDS AND THERAPEUTIC USES THEREOF

The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, diseases associated with over production

Heterocyclic-pyrimindine or pyrazine compound containing biarylamide structure and application thereof

The invention discloses a heterocyclic-pyrimindine or pyrazine compound containing a biarylamide structure. The heterocyclic-pyrimindine or pyrazine compound is as shown in a general formula I or II, wherein the general formula I and the general formula II are shown in the description. The heterocyclic-pyrimindine or pyrazine compound containing the biarylamide structure, and pharmaceutically acceptable salts, hydrates or solvates thereof are used as active components, and are mixed with a pharmaceutically acceptable carrier or excipient to prepare a composition; and the composition is prepared into clinically acceptable preparations. The compound provided by the invention can be used for treating and/or preventing proliferative diseases, and treating and/or preventing prostate cancer, lung cancer and cervical cancer.

The structure containing [...] of thienopyrimidines preparation and application

The invention discloses a thienopyrimidine compound containing a chromone hydrazone structure, a geometrical isomer of the compound, pharmaceutically acceptable salts, hydrates, solvates or prodrugs of the compound, as well as application of the compound to preparation of medicines for treating and/or preventing hyperplastic diseases, application of the compound to preparation of medicines for treating and/or preventing cancers and application of the compound to preparation of medicines for treating and/or preventing lung cancers, liver cancers, gastric cancers, colon cancers and breast cancers.

Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors

Two series of thienopyrimidine derivatives (10a-k, 16a-j) bearing chromone moiety were designed and synthesized. All the compounds were evaluated for inhibitory activity against mTOR kinase at a concentration of 10uM. Four selected compounds were further evaluated for the IC50 values against mTOR kinase, PI3Kα kinase and two cancer cell lines. Some of the target compounds exhibited moderate to excellent mTOR/PI3Kα kinase inhibitory activity and cytotoxicity. The most promising compound 16i showed good inhibitory activity against mTOR/PI3Kα kinase and good antitumor potency for H460 and PC-3 cell lines with IC50 values of 0.16 ± 0.03 μM, 2.35 ± 0.19 μM, 1.20 ± 0.23 μM and 0.85 ± 0.04 μM, which were 8.6, >5, 7.9 and 19.1 times more active than compound I (1.37 ± 0.07 μM, >10 μM, 9.52 ± 0.29 μM, 16.27 ± 0.54 μM), respectively. Structure-activity relationships (SARs) and docking studies indicated that the chromone moiety is necessary for the potent antitumor activity and cytotoxicity of these compounds. Substitution of the chromone moiety at the 6-position has a significant impact to the inhibitory activity, in particular a carboxylic acid group, produced the best potency.

Rational design of phosphoinositide 3-kinase inhibitors that exhibit selectivity over the phosphoinositide 3-kinase isoform

Of the four class I phosphoinositide 3-kinase (PI3K) isoforms, PI3K has justly received the most attention for its potential in cancer therapy. Herein we report our successful approaches to achieve PI3K vs PI3K selectivity for two chemical series. In the thienopyrimidine series of inhibitors, we propose that select ligands achieve selectivity derived from a hydrogen bonding interaction with Arg770 of PI3K that is not attained with the corresponding Lys777 of PI3K. In the benzoxepin series of inhibitors, the selectivity observed can be rationalized by the difference in electrostatic potential between the two isoforms in a given region rather than any specific interaction.

PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE

Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. Formula (Ic) and (Id).