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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis of a new series of 4-chloro-2-mercapto-5-methylbenzenesulfonamide derivatives with potential antitumor activity.
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Synthesis of a new series of 4-chloro-2-mercapto-5-methylbenzenesulfonamide derivatives with potential antitumor activity.

机译：具有潜在抗肿瘤活性的一系列新的4-氯-2-巯基-5-甲基苯磺酰胺衍生物的合成。

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摘要

The syntheses of S-(5-chloro-4-methyl-2-sulfamoylphenyl)alkanethio (or benzothio)hydrazonates (3a-3o) and potassium S-(5-chloro-2-cyanoamidatesulfonyl-4-methylphenyl)alkanethio (or benzothio)hydrazonates (4-10) are described. The compounds 3e, 3i-3o, 7 and 8 were screened at the National Cancer Institute (NCI) for their activities against a panel of 59 tumor cell lines and relationships between structure and antitumor activity in vitro are discussed. The compounds 3e, 3j, 3l-3o and 7 exhibited reasonable activity against numerous human tumor cell lines. The prominent compound 3l showed significant activity against some cell lines of leukemia (SR), melanoma (SK-MEL-5), CNS cancer (SF-539), ovarian cancer (OVCAR-3, OVCAR-4) and breast cancer (MDA-MB-231/ACTT) (GI50 values in the range 0.3-0.9 microM). Furthermore, compound 8 exhibited the high selectivity against renal cancer (A498) cells (GI50 < 0.01 microM, TGI = 2.3 microM and LC50 = 35.7 microM).
机译：S-（5-氯-4-甲基-2-氨磺酰基苯基）烷硫基（或苯硫基）肼基酸酯（3a-3o）和S-（5-氯-2-氰基氨基甲磺酸磺酰基-4-甲基苯基）链烷硫基（或苯硫基）的合成描述了hydr酸盐（4-10）。在美国国家癌症研究所（NCI）筛选了化合物3e，3i-3o，7和8的抗59种肿瘤细胞系的活性，并讨论了体外结构与抗肿瘤活性之间的关系。化合物3e，3j，31-3o和7对许多人肿瘤细胞系表现出合理的活性。突出的化合物3l对白血病（SR），黑素瘤（SK-MEL-5），中枢神经系统癌症（SF-539），卵巢癌（OVCAR-3，OVCAR-4）和乳腺癌（MDA）的某些细胞系表现出显着活性-MB-231 / ACTT）（GI50值在0.3-0.9 microM范围内）。此外，化合物8对肾癌（A498）细胞表现出高选择性（GI50 <0.01 microM，TGI = 2.3 microM和LC50 = 35.7 microM）。

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