1112980-86-5

Usage

Uses

Used in Pharmaceutical Industry:
N-[6-[6-Chloro-5-[[(4-fluorophenyl)sulfonyl]amino]-3-pyridinyl]-1,3-benzothiazol-2-yl]acetamide is used as a precursor in the synthesis of new pharmaceutical compounds for various medical conditions. Its unique structure and functional groups may contribute to the development of drugs with novel mechanisms of action, potentially leading to more effective treatments.
Used in Drug Discovery Research:
In the field of drug discovery, N-[6-[6-Chloro-5-[[(4-fluorophenyl)sulfonyl]amino]-3-pyridinyl]-1,3-benzothiazol-2-yl]acetamide serves as a key compound for exploring its potential biological activities. Researchers can investigate its interactions with various biological targets, such as enzymes, receptors, or ion channels, to understand its therapeutic potential and guide the design of more effective drug candidates.
Used in Medicinal Chemistry:
N-[6-[6-Chloro-5-[[(4-fluorophenyl)sulfonyl]amino]-3-pyridinyl]-1,3-benzothiazol-2-yl]acetamide is utilized in medicinal chemistry for the optimization of drug candidates. By modifying its chemical structure, chemists can fine-tune the compound's pharmacokinetic and pharmacodynamic properties, such as solubility, stability, and bioavailability, to improve its therapeutic efficacy and safety profile.
Used in Drug Development:
As a promising chemical entity, N-[6-[6-Chloro-5-[[(4-fluorophenyl)sulfonyl]amino]-3-pyridinyl]-1,3-benzothiazol-2-yl]acetamide is employed in the drug development process to create new therapeutic agents. It undergoes rigorous testing and evaluation in preclinical and clinical studies to assess its safety, efficacy, and potential side effects, ultimately aiming to bring a new drug to market for the treatment of specific medical conditions.

Upstream product

• 885069-14-7 N-[6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1,3-benzothiazol-2-yl]acetamide 
• 1112982-79-2 N-(5-bromo-2-chloro-3-pyridinyl)-4-fluoro-N-((4-fluorophenyl)sulfonyl)benzenesulfonamide 
• 15864-32-1 2-amino-6-bromobenzothiazole 
• 1112982-88-3 N-(6-(5-amino-6-chloropyridin-3-yl)benzo[d]thiazol-2-yl)acetamide 
• 349-88-2 4-Fluorobenzenesulfonyl chloride 
• 16628-26-5 N-(6-bromo-1,3-benzothiazol-2-yl)acetamide 

Relevant academic research and scientific papers

Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors

Phosphoinositide 3-kinase α (PI3K-α) is a lipid kinase that plays a key regulatory role in several cellular processes. The mutation or amplification of this kinase in humans has been implicated in the growth of multiple tumor types. Consequently, PI3K- has become a target of intense research for drug discovery. Our studies began with the identification of benzothiazole compound 1 from a high throughput screen. Extensive SAR studies led to the discovery of sulfonamide 45 as an early lead, based on its in vitro cellular potency. Subsequent modifications of the central pyrimidine ring dramatically improved enzyme and cellular potency and led to the identification of chloropyridine 70. Further arylsulfonamide SAR studies optimized in vitro clearance and led to the identification of 82 as a potent dual inhibitor of PI3K and mTOR. This molecule exhibited potent enzyme and cell activity, low clearance, and high oral bioavailability. In addition, compound 82 demonstrated tumor growth inhibition in U-87 MG, A549, and HCT116 tumor xenograft models.

PI3 KINASE MODULATORS AND METHODS OF USE

The present invention comprises a new class of compounds capable of modulating the activity of PI3 kinase and, accordingly, useful for treatment of PI3 kinase mediated diseases, including melanomas, carcinomas and other cancer-related conditions. The compounds have a general Formula I wherein each of A1, A2, A3, A4, X, R1 and R2 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of PI3 kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.