451494-91-0

Upstream product

• 367-21-5 3-chloro-4-fluorophenylamine 
• 61032-42-6 methyl 2-amino-4-(benzyloxy)-5-methoxybenzoate 
• 451494-90-9 7-(benzyloxy)-N-(3-chloro-4-flurophenyl)-6-methoxyquinazoline-4-amine 
• 162364-72-9 7-benzyloxy-4-chloro-6-methoxyquinazoline 
• 179688-01-8 7-benzyloxy-6-methoxy-3,4-dihydroquinazolin-4-one 
• 61032-41-5 methyl 4-(benzyloxy)-5-methoxy-2-nitrobenzoate 
• 848092-84-2 methyl 2-amino-4-hydroxy-5-methoxybenzoate 
• 56441-97-5 methyl 4-(benzyloxy)-3-methoxybenzoate 
• 3943-74-6 4-hydroxy-3-methoxybenzoic acid methyl ester 
• 179688-01-8 7-(benzyloxy)-6-methoxyquinazolin-4(3H)-one 
• 179688-03-0 4-chloro-6-methoxyquinazolin-7-yl acetate 
• 179688-02-9 7-acetoxy-6-methoxy-3,4-dihydroquinazolin-4-one 
• 162012-72-8 7-hydroxy-6-methoxy-3,4-dihydroquinazolin-4-one 
• 869475-50-3 acetic acid 4-(3-chloro-4-fluoro-phenylamino)-6-methoxy-quinazolin-7-yl ester 

Downstream Products

• 451494-89-6 trifluoromethanesulfonic acid 4-(3-chloro-4-fluorophenylamino)-6-methoxy-7-quinazolinyl ester 
• 1012061-76-5 ethyl 7-(4-((3-chloro-4-fluorophenyl)amino)-6-methoxyquinazolin-7-yloxy)heptanoate 

Relevant academic research and scientific papers

Fluorescent molecular probe targeting EGFR (epidermal growth factor receptor) as well as preparation method and application of probe

The invention relates to the technical field of molecular probes, and discloses an EGFR (epidermal growth factor receptor) targeting fluorescent molecular probe as well as a preparation method and application of the probe. The fluorescent molecular probe includes a fluorescent labelling group, a connecting group and a reaction group. The reaction group can be combined with EGFR protein in a targeting manner, and specific labeling, tracing and imaging can be carried out through the fluorescence labeling group; and the expression process of specific cells and molecules can be observed in real time by utilizing molecular imaging, and a target point is tracked, so that the evaluation of the disease development condition is realized at the molecular pathological level, and the accurate detection of EGFR mutation typing in lung cancer patients is realized.

Design, synthesis and evaluation of alkylphosphocholine-gefitinib conjugates as multitarget anticancer agents

The evolving resistance to the currently used chemotherapeutic agents requires continuous efforts to develop new anticancer agents overcoming resistance and with lower side effects. Polypharmacology via designing a single molecule intercepting multiple signaling pathways is more effective than targeting a single one. Several alkylphosphocholines show anticancer activity via inhibition of Akt phosphorylation. On the other hand, several molecules having quinazoline scaffold elicit anticancer activity through inhibition of epidermal growth factor receptor (EGFR) tyrosine kinases. We report our efforts to develop alkylphosphocholines-gefitinib conjugates as multitarget anticancer agents. The antiproliferative activities of the newly synthesized compounds were evaluated against cell lines representing lung, breast, liver and skin cancers. In addition, the capability of the newly synthesized compounds to inhibit Akt phosphorylation and EGFR tyrosine kinases were determined. The results emphasized the influence of the linkers’ length on the elicited bioactivity. The long chain linkers possessing conjugates were more active regarding both of the elicited antiproliferative effect and inhibition of Akt phosphorylation, while maintained the ability to inhibit EGFR tyrosine kinases. Their cytotoxic activities were superior or comparable to erlotinib and miltefosine.

QUINAZOLINE DERIVATIVE

Provided are a quinazoline derivative, a pharmaceutical composition containing the same, a method for preparation of said derivative, and an application of same as an anti-cancer drug.

Epidermal growth factor receptor tyrosine kinase inhibitors MPGF and MPGH with anti-tumor activity and preparation method and application thereof

The invention discloses epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKI) MPGF and MPGH with the anti-tumor activity and a preparation method and application thereof. By optimizing and improving the chemical structure of PD153035, brand-new EGFR TKIs are obtained and named as MPGF (shown in the formula I) and MPGH (shown in the formula II). Research shows that the synthesized EGFR TKI-MPGF and EGFR TKI-MPGH can effectively inhibit tumor cell proliferation and has a stronger proliferation inhibition effect on mutational EGFR lung cancer cell line PC-9 compared with the PD153035, and therefore the EGFR TKI-MPGF and the EGFR TKI-MPGH can serve as anti-tumor agents to be applied in clinic. In addition, the invention discloses the method for preparing the epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKI) MPGF and MPGH with the anti-tumor activity. By means of the epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKI) MPGF and MPGH with the anti-tumor activity and the preparation method and application thereof, an effective technological means is provided for tumor treatment, especially for treatment of the non-small cell lung cancer.

Identification of novel 4-anilinoquinazoline derivatives as potent EGFR inhibitors both under normoxia and hypoxia

A novel series of 4-anilinoquinazoline derivatives (19a-19t) were designed and synthesized through incorporation of the 2-nitroimidazole moiety into the 4-anilinoquinazoline scaffold of EGFR inhibitors. The most promising compound 19h displayed potent EGF

Facile synthesis of 7-amino anilinoquinazolines via direct amination of the quinazoline core

The facile preparation of 4-(3-chloro-4-fluoroanilino)-6-alkoxy-7- aminoquinazolines from their corresponding 7-triflate and 7-fluoro precursors are highlighted.

Quinazoline derivatives

A compound of the formula (I) or a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, an optically active compound thereof, a racemate thereof or a diastereomer mixture thereof has a superior tyrosine-specific protein kinase inhibitory activity and is useful as a pharmaceutical agent, particularly as an agent for the prophylaxis or treatment of various cancers, psoriasis or diseases caused by arteriosclerosis, and the like.