69545-37-5

Upstream product

• 728-87-0 4,4'-Dimethoxybenzhydrol 
• 42240-30-2 bis-(4-methoxyphenyl)methyl acetate 
• 90-96-0 bis(p-methoxyphenyl)methanone 
• 123-11-5 4-methoxy-benzaldehyde 
• 104-92-7 1-bromo-4-methoxy-benzene 
• 116664-86-9 bis(4-methoxyphenyl)methyl 4-cyanophenyl ether 
• 46835-92-1 bis(p-methoxyphenyl)methyl cation 

Downstream Products

• 113650-85-4 4-(4,4'-dimethoxy-benzhydryloxy)-1,2,6-trimethyl-piperidine 
• 26608-02-6 bis(4-methoxyphenyl)methanethiol 
• 55681-26-0 α,α-bis(4-methoxyphenyl)acetophenone 
• 918159-83-8 (3S)-(+)-1-di(p-anisyl)methyl-7-chloro-1,3-dihydro-3-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one 
• 334698-95-2 (η5-cyclopentadienyl)dicarbonyl[(1-4-η)-5-phenylcyclohexadiene]molybdenum bromide 
• 1220912-18-4 (ani)2CH-OS(O)Ph 
• 1220912-25-3 di-(4-methoxyphenyl)methyl phenyl sulfone 
• 106864-93-1 β-(bis(4-methoxyphenyl)methanesulfonyl)propionitrile 
• 106864-94-2 β-(bis(4-methoxyphenyl)methylthio)propionitrile 
• 106864-88-4 methyl bis(4-methoxyphenyl)methanesulfinate 
• 150-60-7 dibenzyl disulphide 
• 918159-90-7 (3R)-(-)-1-di(p-anisyl)methyl-3-(N-tert-butoxycarbonyl-indol-3-yl)methyl-7-chloro-1,3-dihydro-3-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one 
• 918160-20-0 (11aR)-(+)-10-di(p-anisyl)methyl-2,3,5,10,11,11a-hexahydro-5,11-dioxo-11a-(2-phenyl)benzyl-1H-pyrrolo[2,1-c][1,4]benzodiazepine 

Relevant academic research and scientific papers

Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with an alkyne spacer as GABA uptake inhibitors

In this study, we present the synthesis and structure–activity relationships (SAR) of novel N-substituted nipecotic acid derivatives closely related to (S)-SNAP-5114 (2) in the pursuit of finding new and potent mGAT4 selective inhibitors. By the use of iminium ion chemistry, a series of new N-substituted nipecotic acid derivatives containing a variety of heterocycles, and an alkyne spacer were synthesized. Biological evaluation of the prepared compounds showed, how the inhibitory potency and subtype selectivity for the murine GABA transporters (mGATs) were influenced by the performed modifications.

Why are vinyl cations sluggish electrophiles?

The kinetics of the reactions of the vinyl cations 2 [Ph2C=C+-(4-MeO-C6H4)] and 3 [Me2C=C+-(4-MeO-C6H4)] (generated by laser flash photolysis) with diverse nucleophile

Substituted diphenyl derivatives

Triazene-substituted diphenyl derivatives are suitable as chemotherapeutic agents for treating carcinomas in humans and animals.

Synthesis and antiproliferative activities of quebecol and its analogs

Simple and efficient synthesis of quebecol and a number of its analogs was accomplished in five steps. The synthesized compounds were evaluated for antiproliferative activities against human cervix adenocarcinoma (HeLa), human ovarian carcinoma (SK-OV-3), human colon carcinoma (HT-29), and human breast adenocarcinoma (MCF-7) cancer cell lines. Among all the compounds, 7c, 7d, 7f, and 8f exhibited antiproliferative activities against four tested cell lines with inhibition over 80% at 75 μM after 72 h, whereas, compound 7b and 7g were more selective towards MCF-7 cell line. The IC50 values for compounds 7c, 7d, and 7f were 85.1 μM, 78.7 μM, and 80.6 μM against MCF-7 cell line, respectively, showing slightly higher antiproliferative activtiy than the synthesized and isolated quebecol with an IC50 value of 104.2 μM against MCF-7.

Nucleofugality and nucleophilicity of fluoride in protic solvents

A series of p-substituted benzhydryl fluorides (diarylfluoromethanes) were prepared and subjected to solvolysis reactions, which were followed conductometrically. The observed first-order rate constants k1(25 °C) were found to follow the correlation equation log k1(25 °C) = sf(Nf + Ef), which allowed us to determine the nucleofuge-specific parameters Nf and sf for fluoride in different aqueous and alcoholic solvents. The rates of the reverse reactions were measured by generating benzhydrylium ions (diarylcarbenium ions) laser flash photolytically in various alcoholic and aqueous solvents in the presence of fluoride ions and monitoring the rate of consumption of the benzhydrylium ions by UV-vis spectroscopy. The resulting second-order rate constants k-1(20 °C) were substituted into the correlation equation log k-1 = sN(N + E) to derive the nucleophilicity parameters N and sN for fluoride in various protic solvents. Complete Gibbs energy profiles for the solvolysis reactions of benzhydryl fluorides are constructed.

TREATMENT OR PROPHYLAXIS OF PROLIFERATIVE CONDITIONS

The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.

Synthesis and anticonvulsant activity of some cinnamylpiperazine derivatives

A series of cinnamylpiperazine derivatives was synthesized using different benzophenone as starting material. The structures of the compounds were proved by their IR, 1H-NMR spectroscopic data and mass spectra data. The anticonvulsant activities of these compounds were evaluated with maximal electroshock (MES) test and rotarod test with intraperitoneal injection on KunMing mice. Among all the flunarizine analogues, no one exhibited better anticonvulsant activity than flunarizine. Flunarizine (4i) exhibited anticonvulsant activity with ED50 of 38.1 mg/kg, TD50 of 164.3 mg/kg and PI of 4.3 through administration intraperitoneal, and with ED50 of 56.8 mg/kg, TD50 of 456.3 mg/kg and PI of 8.0 through oral administration.

Enantioselective synthesis of diversely substituted quaternary 1,4-benzodiazepin-2-ones and 1,4-benzodiazepine-2,5-diones

Benzodiazepines are privileged scaffolds in medicinal chemistry, but enantiopure examples containing quaternary stereogenic centers are extremely rare. We demonstrate that installation of the di-(p-anisyl)methyl (DAM) group at N1 of 1,4-benzodiazepin-2-on

Kinetics of the reactions of halide anions with carbocations: Quantitative energy profiles for SN1 reactions

Rate constants for the reactions of Laser flash photolytically generated benzhydrylium ions (diarylcarbenium ions) with halide ions have been determined in various solvents, including neat and aqueous acetonitrile as well as some alcohols. Substitution of the rate constants into the correlation equation log k = s(N + E) yields the nucleophilicity parameters N for the halide ions in different solvents. Linear correlations with negative slopes are found between the nucleophilicity parameters N for Cl- and Br- in different solvents and the solvent ionizing powers Y of the corresponding solvents. Increasing halide solvation reduces the rates of carbocation/chloride combinations by approximately half as much as it increases the rates of ionizations of benzhydryl chlorides. Comparison of the solvent dependent nucleophilicity parameters N of halide anions and the nucleophilicity parameters N1 for solvents yields a quantitative prediction of common ion rate depression, as demonstrated by the analysis of a variety of literature reported mass-law constants α. Combination of the rate constants for the reactions of benzhydrylium ions with halide ions (k-1) reported in this work with the ionization constants of benzhydryl halides (k1) and the recently reported rate constants for the reactions of benzhydrylium ions with solvents (k2) yields complete quantitative free energy profiles for solvolysis reactions. The applicability of Hammond's postulate for interpreting solvolysis reactions can thus be examined quantitatively.

TARGET-ORIENTED CHEMOTHERAPY FOR TREATING TUMORS OF THE SEXUAL ORGANS

The invention relates to dialkyltriazene-supporting estrogens and antiestrogens that are suited for use as chemotherapeutic drugs for treating carcinomas of the sexual organs of humans and animals.