Thymidine phosphorylase (TP) over expression plays role in several pathological conditions, such as rheumatoid arthritis, chronic inflammatory diseases, psoriasis, and tumor angiogenesis. The inhibitor of this enzyme plays an important role in preventing the serious threat due to over expression of TP. In this regard, a series of seventeenanalogs of 3-formylcoumarin (1–17) were synthesized, characterized by ¹HNMR and EI-MS and screened for thymidine phosphorylaseinhibitory activity. All analogs showed a variable degree of thymidine phosphorylase inhibition with IC₅₀ values ranging between 0.90 ± 0.01 and 53.50 ± 1.20 μM when compared with the standard inhibitor 7-Deazaxanthine having IC₅₀ value 38.68 ± 1.12 μM. Among the series, fifteenanalogs such as 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 15, 16 and 17 showed excellent inhibition which is many folds better than the standard 7-Deazaxanthine whiletwo analogs 13 and 14 showed good inhibition. The structure activity relationship (SAR) was mainly based upon by bring about difference of substituents on phenyl ring. Molecular docking study was carried out to understand the binding interaction of the most active analogs.

胸苷磷酸化酶（TP）的过表达在几种病理状况中起作用，例如类风湿性关节炎，慢性炎性疾病，牛皮癣和肿瘤血管生成。该酶的抑制剂在防止由于TP过度表达引起的严重威胁方面起着重要作用。在这方面，合成了一系列十七个3-甲酰基香豆素的类似物（1 – 17），其特征在于¹ HNMR和EI-MS并筛选了对胸苷磷酸化酶的抑制活性。所有类似物表现出不同程度的胸苷磷酸化酶抑制作用的IC ₅₀值的范围时，7-Deazaxanthine具有IC的标准抑制剂相比0.90和53.50之间μM±0.01±1.20 ₅₀值38.68±1.12μM。在该系列中，十五种类似物，例如1、2、3、4、5、6、7、8、9、10、11、12、15、16和17显示出优异的抑制作用，比标准的7-地氮杂黄嘌呤好很多倍。而两个类似物13和14表现出良好的抑制作用。结构活性关系（SAR）主要基于引起苯环上取代基的差异。进行了分子对接研究以了解最活跃的类似物的结合相互作用。