206192-45-2

Upstream product

• 98-68-0 4-methoxy-phenyl-sulphonyl chloride 
• 85006-31-1 3-amino-4-methyl-2-thiophenecarboxylic acid methyl ester 

Downstream Products

• 206192-49-6 3-[benzyl-(4-methoxy-benzenesulfonyl)-amino]-4-methyl-thiophene-2-carboxylic acid methyl ester 
• 206192-53-2 3-[benzyl-(4-methoxy-benzenesulfonyl)-amino]-4-methyl-thiophene-2-carboxylic acid 

Relevant academic research and scientific papers

Design, structure-activity relationship study and biological evaluation of the thieno[3,2-c]isoquinoline scaffold as a potential anti-cancer agent

Several derivatives of a series that share a thienoisoquinoline scaffold have demonstrated potent activity against cancer cell lines A549, HeLa, HCT-116, and MDA-MB-231 in the submicromolar concentration range. Structure-activity relationship (SAR) studies on a range of derivatives aided in identifying key pharmacophores in the lead compound. A series of compounds have been identified as the most promising with submicromolar IC50 values against a lung cancer cell line (A549). Microscopy studies of cancer cells treated with the lead compound revealed that it causes mitotic arrest and disrupts microtubules. Further evaluation via an in vitro microtubule polymerization assay and competition studies indicate that the lead compound binds to tubulin via the colchicine site.

THIENOISOQUINOLINES AND THEIR DERIVATIVES FOR TARGETING TUBULIN, CH-TOG, AURORA A KINASE, TPX2, CDK5RAP2 AND/OR ASPM

The present disclosure relates to compounds, methods and uses thereof for targeting tubulin, ch-TOG, Aurora A kinase, TPX2, Cdk5rap2 and/or ASPM and for the treatment of cancer in a subject. For example, the compounds can comprise compounds of Formula I or a pharmaceutically acceptable salt, solvate or prodrug thereof. A, Z, RA, RB, R1, R2, R3, R4 and R5 can have different values.

THIENOISOQUINOLINES AND THEIR DERIVATIVES FOR THE TREATMENT OF CANCER

The present disclosure relates to fused N-arylsulfonamidyl-thienoisoquinoline compounds, derivatives and pharmaceutical compositions thereof, and methods and uses in inhibiting cancer cell growth, along with a supplemental anti-cancer agent. Centrosome targeting and microtubule depolymerisation are attractive in designing the present chemotherapeutic compounds. The various diseases and conditions treated include various types of cell cancers, and in vitro inhibition.

HETEROARYL ACETYLENIC SULFONAMIDE AND PHOSPHINIC ACID AMIDE HYDROXAMIC ACID TACE INHIBITORS

Compounds of formula (I) are useful in treating disease conditions mediated by TNF- alpha such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

THE PREPARATION AND USE OF ORTHO-SULFONAMIDO HETEROARYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS

The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF- alpha converting enzyme (TACE, tumor necrosis factor- alpha conve

Heteroaryl acetylenic sulfonamide and phosphinic acid amide hydroxamic acid tace inhibitors

Compounds of the formula: are useful in treating disease conditions mediated by TNF-α such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

Heteroaryl and cycloalkyl sulfonamide hydroxamic acid inhibitors of matrix metalloproteinases

Heteroaryl and cycloalkyl sulfonamide-hydroxamic acid MMP inhibitors were investigated. Of these, the pyridyl analogue 2 is the most potent and selective inhibitor of MMP-9 and MMP-13 in vitro.

PREPARATION AND USE OF ORTHOSULFONAMIDO HETEROARYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITIORS

The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e. g. gelatinases, stromelysins and collagenases) and TNF-α converting enzyme (TACE, tumor necrosis factor-α converting enz