1236153-16-4

Upstream product

• 179688-01-8 7-(benzyloxy)-6-methoxyquinazolin-4(3H)-one 
• 100-39-0 benzyl bromide 
• 56441-97-5 methyl 4-(benzyloxy)-3-methoxybenzoate 
• 61032-41-5 methyl 4-(benzyloxy)-5-methoxy-2-nitrobenzoate 
• 61032-42-6 methyl 2-amino-4-(benzyloxy)-5-methoxybenzoate 
• 3943-74-6 4-hydroxy-3-methoxybenzoic acid methyl ester 
• 372-19-0 meta-fluoroaniline 
• 162364-72-9 7-benzyloxy-4-chloro-6-methoxyquinazoline 

Downstream Products

• 1236153-17-5 C₁₅H₁₂FN₃O₂ 
• 1236153-14-2 4-[(3-fluorophenyl)amino]-6-methoxy-7-(prop-2-ynyloxy)quinazoline 
• 1236153-18-6 4-[(3-fluorophenyl)amino]-6-methoxy-7-(3,6,9,12-tetraoxapentadecan-14-ynyloxy)quinazoline 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel 4-anilinoquinazoline derivatives as hypoxia-selective EGFR and VEGFR-2 dual inhibitors

Tyrosine kinase inhibitors (TKIs) have achieved substantial clinical effects for cancer treatment while causing a number of adverse effects. Since hypoxia is an intrinsic difference between solid tumor and healthy tissues, one strategy to overcome the adverse effects of TKIs is to enhance the specificity of anti-tumor activity by selectively targeting hypoxic region of tumors. Herein, we designed and synthesized a series of novel 4-anilinoquinazoline derivatives by introducing 3-nitro-1,2,4-triazole group to the side chain of vandetanib with modification of aniline moiety. Lead compounds, 10a and 10g, exhibited potent inhibitory activity against EGFR and VEGFR-2 kinase. Moreover, these two compounds were shown to enhance anti-proliferative activities on A549 and H446 cells under hypoxic conditions compared to vandetanib and dramatically down-regulate VEGF gene expression. In vivo studies confirmed that 10a and 10g not only inhibited tumor growth in A549 xenografts of BALB/c-nu mice but also significantly reduce toxicity associated with weight loss compared to vandetanib. These results suggest that EGFR/VEGFR-2 dual inhibitors, 10a and 10g, emerged as potential hypoxia-selective anti-tumor drugs with less toxicity for inhibiting in vitro and in vivo models of non-small cell lung cancer cells.

Synthesis of 6- and 7-propargyloxy derivatives of 4-(3-fluoroanilino)- quinazoline

The preparation of the novel isomeric 6- and 7-propargyloxy derivatives of 4-(3-fluoroanilino)-quinazoline was achieved using a six-step process. An alternate method to the 7-propargyloxy derivative and analogous 7-propargyloxy containing compounds is als

STEROIDAL ANTI-HORMONE HYBRIDS

Disclosed are novel compounds and compositions for inhibition of androgen and estrogen receptor signaling, methods for inhibiting androgen signaling, methods for inhibiting estrogen signaling, methods for inhibiting the interaction between a co-regulatory protein and an androgen or estrogen receptor, and methods for treating cancer.