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Synthesis and antitumor activity of s-tetrazine derivatives.

机译:s-四嗪衍生物的合成及其抗肿瘤活性。

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摘要

Fifty-five compounds of s-tetrazine derivative including hexahydro-, 1,6-dihydro, 1,4-dihydro-, 1,2-dihydro- and aromatic s-tetrazine were prepared. Their antitumor activities were evaluated in vitro by MTT method for P-388 cell and SRB method for A-549 cell. The results show that there are 9 compounds which in 10(-6) microM have more than 50% inhibition rate to A-549 cancer cell growth, and 7 compounds in 10(-6) microM have more than 50% inhibition rate to P-388 cancer cell growth. The IC(50) of compound 3q for P-388, Bel-7402, MCF-7 and A-549 are 0.6 microM, 0.6 microM, 0.5 microM and 0.7 microM, respectively. So s-tetrazine derivative is a kind of compound which possesses potential antitumor activities and is worth to research further.
机译:制备了55种s-四嗪衍生物,包括六氢,1,6-二氢,1,4-二氢,1,2-二氢和芳族s-四嗪。通过MTT法对P-388细胞和SRB法对A-549细胞体外评价其抗肿瘤活性。结果表明,在10(-6)microM中有9种化合物对A-549癌细胞的生长抑制率超过50%,在10(-6)microM中有7种化合物对P的抑制率超过50% -388癌细胞生长。 P-388,Bel-7402,MCF-7和A-549的化合物3q的IC(50)分别为0.6 microM,0.6 microM,0.5 microM和0.7 microM。因此,s-四嗪衍生物是一种具有潜在的抗肿瘤活性的化合物,值得进一步研究。

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