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首页> 外文期刊>Medicinal chemistry >Anti-Cancer Activity of 2,4-Disubstituted Thiophene Derivatives: Dual Inhibitors of Lipoxygenase and Cyclooxygenase
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Anti-Cancer Activity of 2,4-Disubstituted Thiophene Derivatives: Dual Inhibitors of Lipoxygenase and Cyclooxygenase

机译：2,4-二取代噻吩衍生物的抗癌活性：脂氧合酶和环氧合酶的双重抑制剂

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摘要

2,4-Disubstituted thiophene derivatives were synthesized and assessed for anti-inflammatory and anti-cancer activities by targeting two important enzymes of the arachidonic acid metabolism. Both lipoxygenase and cyclooxygenase enzymes play vital role in chronic inflammation and carcinogenesis. Previous studies have proved that COX-2 and 5-LOX are highly activated in various types of cancers; hence inhibition of these clinically important enzymes constitutes the essential criterion for the suppression of tumor progression and metastasis. Among the tested derivatives, 2d and 2g compounds emerged as potent inhibitors of lipoxygenase and cyclooxygenase enzymes. The potent inhibitor of cyclooxygenase was further tested for in vitro cytotoxicity on cervical cancer (HeLa) cells and in vivo tumor model studies using EAT bearing mice where 2-(3,4,5-trimethoxyphenyl)-4-(N-methylindol-3-yl) thiophene (2g) showed eloquent activity. Further, in silico modeling results confirmed the active catalytic ligand binding pockets, which is evident from higher atomic contact energy values of 2d and 2g than compared to standard drug. Thus, 2g may find better application in management of inflammation and in proapoptotic therapeutic engineering.
机译：合成了2，4-二取代噻吩衍生物，并通过靶向花生四烯酸代谢的两种重要酶来评估其抗炎和抗癌活性。脂氧合酶和环氧合酶在慢性炎症和致癌作用中都起着至关重要的作用。先前的研究证明，COX-2和5-LOX在各种类型的癌症中均被高度激活。因此，抑制这些临床上重要的酶构成了抑制肿瘤进展和转移的基本标准。在测试的衍生物中，2d和2g化合物作为脂氧合酶和环氧合酶的有效抑制剂出现。进一步测试了有效的环氧合酶抑制剂对宫颈癌（HeLa）细胞的体外细胞毒性和使用EAT小鼠的体内肿瘤模型研究，其中2-（3,4,5-三甲氧基苯基）-4-（N-甲基吲哚-3 -yl）噻吩（2g）具有雄辩的活性。此外，计算机模拟结果证实了活性催化配体的结合口袋，这从与标准药物相比更高的2d和2g原子接触能值可以看出。因此，2g可能在炎症控制和促凋亡治疗工程中有更好的应用。

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