139210-05-2

Upstream product

• 103-71-9 phenyl isocyanate 
• 138386-58-0 (E)-methyl 3-[2-(triphenylphosphoranylidenamino)phenyl]-propenoate 
• 88939-75-7 methyl (2E)-3-(2-aminophenyl)propenoate 
• 612-41-9 2-nitrocinnamic acid 
• 39228-29-0 (E)-methyl 2-nitrocinnamate 
• 659748-14-8 methyl 3-[2-(3-phenylureido)phenyl]acrylate 
• 138386-58-0 (2E)-3-{2-[(triphenylphosphoranylidene)amino]phenyl}-propenoic acid methyl ester 
• 312913-57-8 (E)-3-[2-(3-Phenyl-ureido)-phenyl]-acrylic acid methyl ester 

Downstream Products

• 115891-42-4 2-anilino-3-carbomethoxyquinoline 
• 928006-44-4 KYS₀₅₀₇₆ 
• 1093791-48-0 C₂₂H₂₈N₄O₂ 
• 1093791-50-4 C₂₇H₃₆N₄O₄ 
• 174534-47-5 4-methoxycarbonylmethyl-2-(1-piperidinyl)-3-phenyl-3,4-dihydroquinazoline 
• 863297-10-3 (2-dimethylamino-3-phenyl-3,4-dihydro-quinazolin-4-yl)-acetic acid methyl ester 
• 659748-16-0 2-phenyl-3,4-dihyroquinazoline 

Relevant academic research and scientific papers

Growth inhibition of human cancer cells in vitro by T-type calcium channel blockers

This paper describes the preliminary biological results that novel T-type calcium channel blockers inhibit the growth of human cancer cells by blocking calcium influx into the cell, based on unknown mechanism on the cell cycle responsible for cellular proliferation. Among the selected compounds from compound library, compound 9c (KYS05041) was identified to be nearly equipotent with Cisplatin against some human cancers in the micromolar range.

3,4-Dihydroquinazoline derivatives inhibit the activities of cholinesterase enzymes

A series of 3,4-dihydroquinazoline derivatives consisting of the selected compounds from our chemical library on the diversity basis and the new synthetic compounds were in vitro tested for their inhibitory activities for both acetylcholinesterase (AChE, from electric eel) and butyrylcholinesterase (BChE, from equine serum) enzymes. It was discovered that most of the compounds displayed weak AChE and strong BuChE inhibitory activities. In particular, compound 8b and 8d were the most active compounds in the series against BChE with IC50 values of 45?nM and 62?nM, as well as 146- and 161-fold higher affinity to BChE, respectively. To understand the excellent activity of these compounds, molecular docking simulations were performed to get better insights into the mechanism of binding of 3,4-dihydroquinazoline derivatives. As expected, compound 8b and 8d bind to both catalytic anionic site (CAS) and peripheral site (PS) of BChE with better interaction energy values than AChE, in agreement with our experimental data. Furthermore, the non-competitive/mixed-type inhibitions of both compounds further confirmed their dual binding nature in kinetic studies.

T-type Ca2+ channel blockers suppress the growth of human cancer cells

In order to further clarify the role of T-type Ca2+ channels in cell proliferation, we have measured the growth inhibition of human cancer cells by using our potent T-type Ca2+ channel blockers. As a result, KYS05090, a most potent T-type Ca2+ channel blocker, was found to be as potent as doxorubicin against some human cancer cells without acute toxicity. Therefore, this letter provides the biological results that T-type calcium channel is important in regulating the important cellular phenotype transition leading to cell proliferation, and thus novel T-type Ca2+ channel blocker presents new prospects for cancer treatment.

Synthesis and SAR study of T-type calcium channel blockers. Part II

3,4-Dihydroquinazoline derivatives have been known to be the novel and potent T-type calcium channel blockers. From a systematic variation of 3,4-dihydroquinazoline derivative 5c (KYS05043), plausible SAR results were established. It was revealed that a 5-(dimethylamino)pentylamino group at R 1, a biphenyl group at R2, and a benzyl amido group at R3 in the 3,4-dihydroquinazoline backbone are closely related with the channel selectivity (T/N-type) as well as the potency based on the discovery of 6k (KYS05090).

Synthesis and SAR studies of a novel series of T-type calcium channel blockers

For the novel, potent, and selective T-type Ca2+ channel blockers, a series of sulfonamido-containing 3,4-dihydroquinazoline derivatives were prepared and evaluated for their blocking actions on T- and N-type Ca2+ channels. Among the

3,4-Dihydroquinazoline derivatives as T-type calcium channel blockers and method of preparing the same

The present invention relates to 3,4-dihydroquinazoline derivatives as T-type calcium channel blockers and a method of preparing the same. The present invention further relates to a composition comprising the same. The composition comprising the 3,4-dihyd

3,4-Dihydroquinazoline derivatives as T-type calcium channel blockers and method of preparing the same

The present invention relates to 3,4-dihydroquinazoline derivatives as T-type calcium channel blockers and a method of preparing the same. The present invention further relates to a composition comprising the same. The composition comprising the 3,4-dihyd

Synthesis of 2-substituted 3,4-dihydroquinazoline derivatives via regioselective addition of a carbon nucleophile to a carbodiimide

Synthesis of 2-alkyl or phenyl-substituted 3,4-dihydroquinazoline derivatives (6) is described via regioselective carbon nucleophilic addition (RMgBr and RM) to a carbodiimide (4) followed by intramolecular conjugate addition.

3,4-Dihydroquinazoline derivatives as novel selective T-type Ca 2+ channel blockers

For LVA T-type Ca2+ channel blockers, 3,4-dihydroquinazoline derivatives as new scaffolds were prepared and evaluated for the inhibitory activity against two members of the recombinant T-type Ca2+ channel family. Among them, 8a (KYS0

Tetrabutylammonium fluoride promoted lntramolecular Nucleophilic attack of a carbodimide group on an α,β-unsaturated ester group

(N-Aryl, N'-aryl/alkyl) carbodiimides bearing an α,βunsaturated ester moiety in the ortho position undergo cyclization in the presence of tetrabutylammonium fluoride under mild conditions to give dihydroquinazoline derivatives in synthetically useful yields.