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新型 3-烯丙基硫代-6-(单或双取代)氨基嘧啶的合成及抗癌活性。

Synthesis and anticancer activities of new 3-allylthio-6-(mono or disubstituted)aminopyridazines.

机构信息

Pharmaceutical Research Institute, Kwang Dong Pharmaceutical Co., Ltd, Pyong-Taek 459-020, Korea.

出版信息

Arch Pharm Res. 2010 Feb;33(2):189-96. doi: 10.1007/s12272-010-0201-x. Epub 2010 Feb 24.

Abstract

A new series of 3-allylthio-6-(mono or disubstituted) aminopyridazines was synthesized by reacting 3-allylthio-6-chloropyridazine with several amines to develop new anticancer agents. These new compounds showed antiproliferative activities against lung cancer (A549), hepatoblastoma (Hep3b), prostate cancer (PC3), colon cancer (SW480) and cervical cancer (HeLa) cells in MTT assays, and could be promising candidates for chemotherapy of carcinomas. Compound 5 (3-allylthio-6-homopiperidinylaminopyridazine) showed higher potencies than 5-FU for inhibiting the growth of these cell lines. This suggests the potential anticancer activity of compound 5.

摘要

新的一系列 3-烯丙基硫代-6-(单或双取代)氨基哒嗪是通过将 3-烯丙基硫代-6-氯哒嗪与几种胺反应合成的,以开发新的抗癌药物。这些新化合物在 MTT 测定中对肺癌 (A549)、肝母细胞瘤 (Hep3b)、前列腺癌 (PC3)、结肠癌 (SW480) 和宫颈癌 (HeLa) 细胞显示出抗增殖活性,可能是癌症化疗的有希望的候选药物。化合物 5(3-烯丙基硫代-6-高哌啶基氨基哒嗪)对抑制这些细胞系的生长表现出比 5-FU 更高的效力。这表明化合物 5 具有潜在的抗癌活性。

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