对苯二甲酸的细胞毒性苄基酰肼及其相关化合物。

M. Hossain, S. C. Hall, P. J. Wiggington, S. Roth, S. Das, U. Das, P. K. Roayapalley, J. Dimmock
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引用次数: 1

摘要

本研究涉及合成一些新型苄基肼作为候选细胞毒性药物。以对苯二甲酸和间苯二甲酸为原料制备这些化合物的过程令人满意。然而,邻苯二甲酸肼与各种芳醛的反应一般都不成功。发现了一些意想不到的产品。测定了三个具有代表性的化合物1b、2b和3b的芳基环B和C中心的形状和距离。对化合物1a-e、2a-e和3b进行了抗人HCT116和HT29结肠癌细胞以及人CRL1790非恶性结肠癌细胞的筛选,发现这些化合物具有肿瘤选择性毒性。
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Cytotoxic benzylidene hydrazides of terephthalic acid and related compounds.
The present investigation involved the synthesis of a number of novel benzylidene hydrazides as candidate cytotoxic agents. The preparation of these compounds from terephthalic acid and isophthalic acid proceeded satisfactorily. However, the reaction of phthalic acid hydrazide with various aryl aldehydes was unsuccessful in general. Some of the unexpected products were identified. The shapes and also the distances between the centers of the aryl rings designated B and C of three representative compounds 1b, 2b and 3b were determined. The compounds designated 1a-e, 2a-e and 3b were screened against human HCT116 and HT29 colon cancer cells as well as human CRL1790 non-malignant colon cells which revealed the tumor-selective toxicity displayed by these compounds.
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