51193-27-2

Upstream product

• 20893-76-9 Biphenyl-3-diazonium; chloride 
• 1004539-95-0 S-(biphenyl-3-yl) O-ethyl dithiocarbonate 
• 66738-30-5 O-3-Biphenylyl-N,N-dimethyl-thiocarbamat 
• 2113-57-7 3-bromobiphenyl 
• 2113-55-5 3-phenylaniline hydrochloride 
• 2243-47-2 3-biphenyl amine 

Downstream Products

• 109880-88-8 o-(biphenyl-3-ylthio)benzophenone 
• 785817-37-0 N-(8-{[([1,1'-biphenyl]-3-yl)sulfanyl]methyl}-3,4-dihydro-6-nitro-4-oxoquinazolin-2-yl)-2,2-dimethylpropanamide 
• 944705-79-7 3-(3-phenylphenylthio)-N-(4-cyano-3-(trifluoromethyl)phenyl)-2-hydroxy-2-methylpropanamide 
• 785817-56-3 N-(6-amino-8-{[([1,1'-biphenyl]-3-yl)sulfanyl]methyl}-3,4-dihydro-4-oxoquinazolin-2-yl)-2,2-dimethylpropanamide 
• 72001-26-4 3,9-diphenyl-thioxanthene 
• 72001-27-5 3,9,9-diphenyl-thioxanthene 
• 109880-89-9 3,9-diphenylthioxanthenol 
• 109880-94-6 o-(biphenyl-3-ylthio)phenyl(diphenyl)methanol 
• 1311195-73-9 3-(3,4,5-trimethoxyphenylsulfinyl)biphenyl 
• 1311195-72-8 3-(3,4,5-trimethoxyphenylsulfonyl)biphenyl 

Relevant academic research and scientific papers

2-Aminomethylene-5-sulfonylthiazole Inhibitors of Lysyl Oxidase (LOX) and LOXL2 Show Significant Efficacy in Delaying Tumor Growth

The lysyl oxidase (LOX) family of extracellular proteins plays a vital role in catalyzing the formation of cross-links in fibrillar elastin and collagens leading to extracellular matrix (ECM) stabilization. These enzymes have also been implicated in tumor progression and metastatic disease and have thus become an attractive therapeutic target for many types of invasive cancers. Following our recently published work on the discovery of aminomethylenethiophenes (AMTs) as potent, orally bioavailable LOX/LOXL2 inhibitors, we report herein the discovery of a series of dual LOX/LOXL2 inhibitors, as well as a subseries of LOXL2-selective inhibitors, bearing an aminomethylenethiazole (AMTz) scaffold. Incorporation of a thiazole core leads to improved potency toward LOXL2 inhibition via an irreversible binding mode of inhibition. SAR studies have enabled the discovery of a predictive 3DQSAR model. Lead AMTz inhibitors exhibit improved pharmacokinetic properties and excellent antitumor efficacy, with significantly reduced tumor growth in a spontaneous breast cancer genetically engineered mouse model.

Design, synthesis, and SAR studies of 4-substituted methoxylbenzoyl-aryl- thiazoles analogues as potent and orally bioavailable anticancer agents

In a continued effort to improve upon the previously published 4-substituted methoxybenzoyl-aryl-thiazole (SMART) template, we explored chemodiverse "B" rings and "B" to "C" ring linkage. Further, to overcome the poor aqueous solubility of this series of agents, we introduced polar and ionizable hydrophilic groups to obtain water-soluble compounds. For instance, based on in vivo pharmacokinetic (PK) studies, an orally bioavailable phenyl-amino-thiazole (PAT) template was designed and synthesized in which an amino linkage was inserted between "A" and "B" rings of compound 1. The PAT template maintained nanomolar (nM) range potency against cancer cell lines via inhibiting tubulin polymerization and was not susceptible to P-glycoprotein mediated multidrug resistance in vitro, and markedly improved solubility and bioavailability compared with the SMART template (45a-c (PAT) vs 1 (SMART)).

COMPOUNDS FOR TREATMENT OF CANCER

The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.

PAN-ANTAGONISTS FOR THE ANDROGEN RECEPTOR AND ANDROGEN RECEPTOR MUTANTS ASSOCIATED WITH ANTI-ANDROGEN WITHDRAWAL

Disclosed herein are novel antagonists of the androgen receptor and androgen receptor mutations associated with clinical failure of currently prescribed anti-androgens and use of said antagonists in the treatment of conditions associated with inappropriat

Circumventing anti-androgen resistance by molecular design

Nuclear/steroid hormone receptors (NHRs) function as ligand-dependent transcriptional regulators of diverse sets of genes involved in development and homeostasis. Mutations to the androgen receptor (AR), a member of NHRs, have been linked to the failure o

The synthesis of new 2,4-diaminofuro[2,3-d]pyrimidines with 5-biphenyl, phenoxyphenyl and tricyclic substitutions as dihydrofolate reductase inhibitors

Nonclassical 2,4-diamino-5-substituted furo[2,3-d]pyrimidines 4a-i, 5a-b and 7a-f were synthesized as extended aromatic ring appended analogs of previously reported antifolates 1a-b. The extended aromatic system was designed to better interact with a phenylalanine residue (Phe69) of dihydrofolate reductase from the opportunistic pathogen Pneumocystis carinii to afford potent and selective inhibitors of Pneumocystis carinii dihydrofolate reductase. The target compounds were synthesized by nucleophilic displacement of 2,4-diamino-5-(chloromethyl)furo[2,3-d]pyrimidine 3 with the appropriate aromatic amine or thiol. The compounds were evaluated as inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii, and their selectivity was determined using rat liver dihydrofolate reductase as the mammalian reference. In the C8-N9 bridged series, compound 4e, with a 3-(2-methoxydibenzofuran)- side chain, exhibited greatest potency and was more than 3 times as selective for Pneumocystis carinii dihydrofolate reductase compared to rat liver dihydrofolate reductase. Compounds 4b and 4c also exhibited selectivity. Compounds in the C8-S9 bridged series showed comparable potencies, and each showed higher selectivity for Pneumocystis carinii dihydrofolate reductase compared to rat liver dihydrofolate reductase.

10-Thia-anthracenes. Part 3. A Re-examination of the Reaction of 9-Phenylthioxanthylium Salt and Phenyl-lithium

Reaction of 9-phenylthioxanthylium salt (1) with phenyl-lithium afforded eight compounds, 9-phenyl- (2), 9,9-diphenyl- (3). 3,9-diphenyl (4), 3,9,9-triphenyl- (5), and 4,9,9-triphenyl-thioxanthene (6), 9,9'-diphenyl-9,9'-bithioxanthenyl (7), thioxanthone (8), and 9,9'-diphenyldithioxanth-9-yl peroxide (9).Their structures were determined by comparison with the authentic samples.Six samples, (3)-(6), 2,9,9-triphenyl- (30), 9-(biphenyl-4-yl)-9-phenylthioxanthene (31) were independently synthesized in order to determine the structures of two pairs of positional isomers, 3,4, and 5,6.A radical mechanism contributed to the reaction of compound (1) with phenyl-lithium.