首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >One pot synthesis of thiazolodihydropyrimidinones and evaluation of their anticancer activity.
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One pot synthesis of thiazolodihydropyrimidinones and evaluation of their anticancer activity.

机译:一锅合成噻唑二氢嘧啶酮并评估其抗癌活性。

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摘要

2-(5-Arylfurfurylidene/5-nitrofurfurylidene)-5-aryl-7-(2,4-dichloro-5-fluo rophenyl)-5H-thiazolo[2,3-b]-pyrimidin-2(1H)-ones 5 and 6 are synthesized by a novel three component reaction of 4,6-diarylpyrimidino-2(1H)-thiones 4, monochloroacetic acid, arylfurfuraldehydes and 5-nitro-2-furfuraldenediacetate, respectively. The newly synthesized compounds are characterized by elemental analysis, IR, (1)H NMR and mass spectral studies. These compounds exhibited in vitro antitumour activity with moderate to excellent growth inhibition against a panel of 60 cell lines of leukemia, non-small cell lung cancer melanoma, ovarian cancer, prostate cancer and breast cancer.
机译:2-(5-芳基糠叉基/ 5-硝基糠叉基)-5-芳基-7-(2,4-二氯-5-氟苯基)-5H-噻唑并[2,3-b]-嘧啶-2(1H)-ones分别通过4,6-二芳基嘧啶基-2(1H)-硫酮4,一氯乙酸,芳基糠醛和5-硝基-2-糠醛二乙酸酯的新型三组分反应合成图5和6。通过元素分析,IR,(1)H NMR和质谱研究对新合成的化合物进行表征。这些化合物对白血病,非小细胞肺癌黑素瘤,卵巢癌,前列腺癌和乳腺癌等60种细胞系显示出体外抗肿瘤活性,并具有中等至优异的生长抑制作用。

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