34259-86-4

Upstream product

• 41979-39-9 4-piperidone hydrochloride 
• 98-09-9 benzenesulfonyl chloride 
• 41661-47-6 piperidin-4-one 
• 108-98-5 thiophenol 
• 177-11-7 4,4-ethylenedioxy-piperidine 
• 609785-04-8 8-(phenylsulfonyl)-1,4-dioxa-8-azaspiro[4.5]decane 

Downstream Products

• 196882-97-0 4-methoxy-1-(phenylsulfonyl)-1,2,3,6-tetrahydropyridine 
• 196882-99-2 2,5-bis-benzenesulfonyl-8-hydroxy-7-methoxy-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole 
• 267666-53-5 5-benzenesulfonyl-7-methoxy-5H-pyrido[4,3-b]indole 
• 267666-59-1 5-benzenesulfonyl-7-methoxy-5H-pyrido[4,3-b]indole 2-oxide 
• 267666-68-2 5-benzenesulfonyl-1-chloro-7-methoxy-5H-pyrido[4,3-b]indole 
• 267666-52-4 5-benzenesulfonyl-7,8-dimethoxy-5H-pyrido[4,3-b]indole 
• 267666-58-0 5-benzenesulfonyl-7,8-dimethoxy-5H-pyrido[4,3-b]indole 2-oxide 
• 267666-67-1 5-benzenesulfonyl-1-chloro-7,8-dimethoxy-5H-pyrido[4,3-b]indole 
• 267666-45-5 2,5-bis-benzenesulfonyl-7-methoxy-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole 
• 267666-36-4 2,5-bis-benzenesulfonyl-7,8-dimethoxy-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole 
• 267666-42-2 trifluoromethanesulfonic acid 2,5-bis-benzenesulfonyl-7-methoxy-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-8-yl ester 
• 1020002-80-5 C₂₂H₂₉NO₅S 

Relevant academic research and scientific papers

THERAPEUTICS TARGETING MUTANT ADENOMATOUS POLYPOSIS COLI (APC) FOR THE TREATMENT OF CANCER

The present disclosure reports an extensive medicinal chemistry evaluation of a large collection of Truncating APC-Selective Inhibitor (TASIN) compounds. The compounds were evaluated for activity against a series of colon cancer cell lines with and withou

Design and Synthesis of TASIN Analogues Specifically Targeting Colorectal Cancer Cell Lines with Mutant Adenomatous Polyposis Coli (APC)

Despite advances in targeted anticancer therapies, there are still no small-molecule-based therapies available that specifically target colorectal cancer (CRC) development and progression, the second leading cause of cancer deaths. We previously disclosed the discovery of truncating adenomatous polyposis coli (APC)-selective inhibitor 1 (TASIN-1), a small molecule that specifically targets colorectal cancer cells lines with truncating mutations in the adenomatous polyposis coli (APC) tumor suppressor gene through inhibition of cholesterol biosynthesis. Here, we report a medicinal chemistry evaluation of a collection of TASIN analogues and activity against colon cancer cell lines and an isogenic cell line pair reporting on the status of APC-dependent selectivity. A number of potent and selective analogues were identified, including compounds with good metabolic stability and pharmacokinetic properties. The compounds reported herein represent a first-in-class genotype-selective series that specifically target apc mutations present in the majority of CRC patients and serve as a translational platform toward a targeted therapy for colon cancer.

Sulfonamide Synthesis through Electrochemical Oxidative Coupling of Amines and Thiols

Sulfonamides are key motifs in pharmaceuticals and agrochemicals, spurring the continuous development of novel and efficient synthetic methods to access these functional groups. Herein, we report an environmentally benign electrochemical method which enables the oxidative coupling between thiols and amines, two readily available and inexpensive commodity chemicals. The transformation is completely driven by electricity, does not require any sacrificial reagent or additional catalysts and can be carried out in only 5 min. Hydrogen is formed as a benign byproduct at the counter electrode. Owing to the mild reaction conditions, the reaction displays a broad substrate scope and functional group compatibility.

Sulfonamide Synthesis through Electrochemical Oxidative Coupling of Amines and Thiols

Sulfonamides are key motifs in pharmaceuticals and agrochemicals, spurring the continuous development of novel and efficient synthetic methods to access these functional groups. Herein, we report an environmentally benign electrochemical method which enables the oxidative coupling between thiols and amines, two readily available and inexpensive commodity chemicals. The transformation is completely driven by electricity, does not require any sacrificial reagent or additional catalysts and can be carried out in only 5 min. Hydrogen is formed as a benign byproduct at the counter electrode. Owing to the mild reaction conditions, the reaction displays a broad substrate scope and functional group compatibility.

THERAPEUTICS TARGETING TRUNCATED ADENOMATOUS POLYPOSIS COLI (APC) PROTEINS

The described invention provides small molecule anti-cancer compounds that selectively target and inhibit measurable biological activity of truncated APC proteins, an immortalized Human Colonic Epithelial Cell (HCEC) model, and pharmaceutical compositions comprising at least one of the small molecule anti-cancer compounds and a pharmaceutically acceptable carrier.

Novel 3,5-bis(arylidiene)-4-piperidone based monocarbonyl analogs of curcumin: Anticancer activity evaluation and mode of action study

A series of eighteen novel 3,5-bis(arylidiene)-4-piperidone based symmetrical monocarbonyl analogs of curcumin were synthesised and a subset was screened by National Cancer Institute (NCI), USA for their anticancer activity. Dose-response studies and the

Synthesis and antimalarial-activity evaluation of tetraoxane-triazine hybrids and spiro[piperidine-4,3′-tetraoxanes]

A series of tetraoxane-triazine hybrids and spiro[piperidine-4,3′- tetraoxanes] have been synthesized, and all the compounds were screened for in vitro antimalarial activity against chloroquine-sensitive (D6) and chloroquine-resistant (W2) strains of Plas

NOVEL ANALGESIC THAT BINDS FILAMIN A

A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula I, wherein R1 and R2 are substituents, and n, W, X and Y are defined within.

Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles

A rapid, two-step synthesis of a range of dispiro-1,2,4,5-tetraoxanes with potent antimalarial activity both in vitro and in vivo has been achieved. These 1,2,4,5-tetraoxanes have been proven to be superior to 1,2,4-trioxolanes in terms of stability and to be superior to trioxane analogues in terms of both stability and activity. Selected analogues have in vitro nanomolar antimalarial activity and good oral activity and are nontoxic in screens for both cytotoxicity and genotoxicity. The synthesis of a fluorescent 7-nitrobenza-2-oxa-1,3-diazole (NBD) tagged tetraoxane probe and use of laser scanning confocal microscopy techniques have shown that tagged molecules accumulate selectively only in parasite infected erythrocytes and that intraparasitic formation of adducts could be inhibited by co-incubation with the iron chelator desferrioxamine (DFO).

Piperidine dispiro-1,2,4-trioxane analogues

Dispiro N-Boc-protected 1,2,4-trioxane 2 was synthesised via Mo(acac)2 catalysed perhydrolysis of N-Boc spirooxirane followed by condensation of the resulting β-hydroperoxy alcohol 10 with 2-adamantanone. N-Boc 1,2,4-trioxane 2 was converted to the amine 1,2,4-trioxane hydrochloride salt 3 which was subsequently used to prepare derivatives (4-7). Several of these novel 1,2,4-trioxanes had nanomolar antimalarial activity versus the 3D7 strain of Plasmodium falciparum. Amine intermediate 3 represents a versatile derivative for the preparation of achiral arrays of trioxane analogues with antimalarial activity.