35481-04-0

Upstream product

• 97-15-4 4-methyl-N-(2-methyl-4-nitrophenyl)benzenesulfonamide 
• 99-52-5 2-methyl-4-nitro-benzenamine 
• 98-59-9 p-toluenesulfonyl chloride 

Relevant academic research and scientific papers

Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia

A new series of diphenylpyrimidine derivatives (SFA-DPPYs) were synthesized by introducing a functional sulfonamide into the C-2 aniline moiety of pyrimidine template, and then were biologically evaluated as potent Bruton's tyrosine kinase (BTK) inhibitors. Among these molecules, inhibitors 10c, 10i, 10j and 10k displayed high potency against the BTK enzyme, with IC50 values of 1.18?nM, 0.92?nM, 0.42?nM and 1.05?nM, respectively. In particular, compound 10c could remarkably inhibit the proliferation of the B lymphoma cell lines at concentrations of 6.49?μM (Ramos cells) and 13.2?μM (Raji cells), and was stronger than the novel agent spebrutinib. In addition, the inhibitory potency toward the normal PBMC cells showed that inhibitor 10c possesses low cell cytotoxicity. All these explorations indicated that molecule 10c could serve as a valuable inhibitor for B-cell lymphoblastic leukemia treatment.

Design, synthesis and biological evaluation of sulfonamide-substituted diphenylpyrimidine derivatives (Sul-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with antitumor activity

A class of sulfonamide-substituted diphenylpyrimidines (Sul-DPPYs) were synthesized to improve activity against the focal adhesion kinase (FAK). Most of these new Sul-DPPYs displayed moderate activity against the FAK enzyme with IC50 values of less than 100?nM; regardless, they could effectively inhibit several classes of refractory cancer cell lines with IC50 values of less than 10?μM, including the pancreatic cancer cell lines (AsPC-1, Panc-1 and BxPC-3), the NSCLC-resistant H1975 cell line, and the B lymphocyte cell line (Ramos cells). Results of flow cytometry indicated that inhibitor 7e promoted apoptosis of pancreatic cancer cells in a dose-dependent manner. In addition, it almost completely induced the apoptosis at a concentration of 10?μM. Compound 7e may be selected as a potent FAK inhibitor for the treatment of pancreatic cancer.

AROMATIC SULFONE COMPOUND AS ALDOSTERONE RECEPTOR MODULATOR

The present invention provides a compound represented by the following formula (I): [wherein, A represents a group of the following formula (A-1): etc., R1 and R2 each independently represent a hydrogen atom etc., Z represents CR3 etc., W represents CR4 etc., Q represents CR5 etc., R3, R4 and R5 each independently represent a hydrogen atom etc., Y represents an oxygen atom or sulfur atom, X represents an oxygen atom etc. and B represents an optionally substituted aryl group or optionally substituted heteroaryl group], the prodrug thereof or the pharmaceutically acceptable salt thereof for preventing or treating various diseases such as hypertesion, cerebral stroke, cardiac failure, etc.

Process for preparing 4-amino-3-methyl-N-substituted or unsubstituted alkylanilines

A process for the preparation of 4-amino-3-methyl-N-substituted or unsubstituted alkylanilines comprising acylating and/or sulfonylating 4-amino-3-methyl-nitro-benzene having the formula (I) STR1 with an acylation or sulfonylation agent to obtain a compound having the general formula (II) STR2 wherein R1 represents a hydrogen atom or an acyl group, R2 represents an acyl group or a sulfonyl group, or R1 and R2 can combine as a difunctional acyl group; reducing the nitro group of the compound having the general formula (II) with hydrogen in the presence of a metal hydrogenation catalyst to obtain a compound having the general formula (III) STR3 wherein R1 and R2 are as above defined; alkylating the amino group of the compound having the general formula (III) with an alkylation agent selected from the group consisting of an alkyl halide, a substituted alkyl halide and an alkylene oxide to obtain a compound having the general formula (IV) STR4 wherein R1 and R2 are as above defined, R3 represents an alkyl group or a substituted alkyl group and R4 represents a hydrogen atom, an alkyl group or a substituted alkyl group; and hydrolyzing the compound having the general formula (IV) to obtain a compound having the general formula (V) STR5 wherein R3 and R4 are as above defined.