1353659-91-2

Upstream product

• 106-49-0 p-toluidine 
• 1353659-90-1 (E)-3-ethoxy-N-(4-methylphenyl)acryamide 
• 17356-08-0 thiourea 
• 1427163-18-5 C₁₂H₁₆BrNO₃ 

Downstream Products

• 1427163-04-9 N-(4-methylphenyl)-2-(2-(pyrrolidin-1-yl)acetamido)thiazole-5-carboxamide 
• 1427163-12-9 N-(4-methylphenyl)-2-(2-(piperidin-1-yl)acetamido)thiazole-5-carboxamide 
• 1427162-41-1 N-(4-methylphenyl)-2-(2-morpholinoacetamido)thiazole-5-carboxamide 
• 1427162-28-4 N-(4-methylphenyl)-2-(2-(4-methylpiperazin-1-yl)acetamido)thiazole-5-carboxamide 
• 1427162-58-0 N-(4-methylphenyl)-2-(2-(4-(2-hydroxyethyl)piperazin-1-yl)acetamido)thiazole-5-carboxamide 
• 1427162-77-3 2-(2-(azepan-1-yl)acetamido)-N-(4-methylphenyl)thiazole-5-carboxamide 
• 1427163-25-4 C₁₃H₁₂ClN₃O₂S 

Relevant academic research and scientific papers

2-Aminoxazole and 2-Aminothiazole Dasatinib Derivatives as Potent Inhibitors of Chronic Myeloid Leukemia K562 Cells

Dasatinib is an important drug against chronic myeloid leukemia (CML). In this paper, we describe the preparation and anti-CML activity of 2-aminoxazole and 2-aminothiazole dasatinib derivatives. Biological activity was measured by the inhibition of proliferation of human CML K562 cells. The 2-aminoxazole derivatives had similar activities as the 2-aminothiazole derivatives. All newly synthesized compounds demonstrated more potent antiproliferative activity than imatinib. A few compounds (8b, 8c, 9b) showed nanomolar inhibitory activity, similar to that of dasatinib.

Synthesis of 2-aminoxazole-5-carbamides and 2-aminothiazole-5-carbamides as potent inhibitors of CML

Abstract 2-Aminoxazole-5-carbamide was discovered as novel potent inhibitor against human chronic myeloid leukemia K562 cells; several new corresponding 2-aminothiazole-5-carbamides were also prepared and evaluated the biological activity. The results dem

Design, synthesis and antiproliferative activity of 2-acetamidothiazole-5- carboxamide derivatives

In order to develop a new series of dual inhibitors of SRC and ABL, and to investigate whether the pyrimidin-4-ylamino moiety is critical for dasatinib's activity, acetyl substitution was adopted as alternate scaffold at the 2-amino group. Eighteen novel dasatinib derivatives were developed by a parallel synthesis approach and evaluated for their antiproliferative effects. Preliminary tests showed that some of the target compounds IId, IIe and IIf manifested strong antiproliferative activity against MCF-7, MDA-MB 231 and HT-29 cells. Easpecially IId proved to be the most potent compound. Structure-activity relationship studies indicate that the introduction of acetyl substitution as alternate scaffold of pyrimidin-4-ylamino reduced the activity.