138386-58-0

Upstream product

• 88939-75-7 methyl (2E)-3-(2-aminophenyl)propenoate 
• 603-35-0 triphenylphosphine 
• 88939-75-7 methyl β-(o-aminophenyl)acrylate 
• 612-41-9 2-nitrocinnamic acid 
• 39228-29-0 methyl 2-nitrocinnamate 

Downstream Products

• 139210-15-4 (E)-3-[2-((E)-Styryliminomethyleneamino)-phenyl]-acrylic acid methyl ester 
• 139210-05-2 (E)-3-(2-Phenyliminomethyleneamino-phenyl)-acrylic acid methyl ester 
• 139210-07-4 (E)-3-(2-p-Tolyliminomethyleneamino-phenyl)-acrylic acid methyl ester 
• 115891-42-4 2-anilino-3-carbomethoxyquinoline 
• 138386-80-8 2-p-Tolylamino-quinoline-3-carboxylic acid methyl ester 
• 138386-83-1 3-Phenyl-9H-pyrido[2,3-b]indole-4-carboxylic acid methyl ester 
• 138386-84-2 3-(4-Methoxy-phenyl)-9H-pyrido[2,3-b]indole-4-carboxylic acid methyl ester 
• 839672-50-3 methyl 3-[2-((4-biphenyl)iminomethyleneamino)phenyl]acrylate 
• 928006-45-5 KYS₀₅₀₇₉ 
• 955009-86-6 3-biphenyl-4-yl-2-[(5-N,N-dibenzylaminopentyl)-N'-methylamino]-4-methoxycarbonylmethyl-3,4-dihydroquinazoline 
• 955011-81-1 KYS₀₅₀₈₉ 
• 1076689-75-2 2-[N-(5-aminopentyl)-N-methylamino]-3-(4-biphenylyl)-4-methoxycarbonylmethyl-3,4-dihydroquinazoline 
• 1076689-73-0 4-(N-benzylacetamino)-3-(4-biphenylyl)-2-[N-(5-aminopentyl)-N-methylamino]-3,4-dihydroquinazoline 
• 139210-17-6 (E)-3-[2-(Furan-2-yliminomethyleneamino)-phenyl]-acrylic acid methyl ester 

Relevant academic research and scientific papers

Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice

In the previous article we have reported that 3,4-dihydroquinazoline 1 is a potent and selective T-type calcium channel blocker that exhibited strong anti-cancer activity in vitro. Compound 1·2HCl was further in vivo evaluated against A549 xenograft in BALB/c nude mice, which exhibited 49% tumor-weight inhibition through intravenous administration of 2 mg/kg of body weight and was more potent than doxorubicin. Moreover, compound 1·2HCl has an oral bioavailability of 98% with LD50 values of 693 mg/kg (po route) and 40.0 mg/kg (iv route) of body weight. In addition, its efficient scale-up synthetic method was developed.

Quinolines from Morita-Baylis-Hillman acetates of 2-azidobenzaldehydes

A simple method for synthesizing several 2-alkoxy-3-arylsulfinylmethylquinolines using an aza-Wittig type reaction of 3-(2-azidophenyl)-2-(arylsulfinylmethyl)propenoates, which were readily obtained from the Morita-Baylis-Hillman acetates of 2-azidobenzal

3,4-DIHYDROQUINAZOLINE DERIVATIVES

The present invention relates to 3,4-dihydroquinazoline derivatives, a process of preparing them and a pharmaceutical composition including them. The 3,4-dihydroquinazoline derivatives of the present invention have excellent T-type calcium channel blocking effect and anti-cancer activity.

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).

2-(3-Phenyl-2-piperazinyl-3,4-dihydroquinazolin-4-yl)acetic acids as antiviral agents, especially against cytomegaloviruses

The invention relates to dihydroquinazolines and methods for the production thereof, the use thereof in the treatment and/or prophylaxis of diseases, in addition to the use thereof in the production of medicaments in the treatment and/or prophylaxis of diseases, especially for use as anti-viral agents, especially against cytomegalo viruses.

Discovery of potent T-type calcium channel blocker

The intensive SAR study of 3,4-dihydroquinazoline series led to the most potent compound 10 (KYS05090: IC50 = 41 ± 1 nM) against T-type calcium channel and its potency is nearly comparable to that of Kurtoxin. As a small organic molecule, this compound showed the highest blocking activity reported to date.

Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers

We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type Ca2+ channel blockers and evaluated for their inhibitory activities against two subtypes T-type Ca2+ channels and N-type Ca2+ chann

2-(3-PHENYL-2-PIPERAZINYL-3,4-DIHYDROQUINAZOLINE-4-YL) ACETIC ACIDS AS ANTI-VIRAL AGENTS, ESPECIALLY AGAINST CYTOMEGALO VIRUSES

The invention relates to dihydroquinazolines and methods for the production thereof, the use thereof in the treatment and/or prophylaxis of diseases, in addition to the use thereof in the production of medicaments in the treatment and/or prophylaxis of diseases, especially for use as anti-viral agents, especially against cytomegalo viruses.