Synthesis and antiproliferative activity of novel A-homo-B-norsteroid thiadiazole derivatives |
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| Authors: | Yanmin Huang Chunhui Yang Junyan Zhan Chunfang Gan Zhiping Liu Chunling Pang Haifeng Chen Jianguo Cui |
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| Institution: | 1. College of Chemistry and Material Science, Guangxi Teachers Education University, Nanning 530001, China;2. Guangxi Colleges and University Key Laboratory of Beibu Gulf Oil and Natural Gas Resource Effective Utilization, Qizhou University, China |
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| Abstract: | Using cholesterol as a starting material, two novel steroidal thiadiazole derivatives possessing a structure of A-homo lactam and a B-nor steroidal skeleton were designed and synthesized by six steps of reactions, and their antiproliferative activities were assayed against various cancer cell lines. The result shows that compound 7b displays an excellent selective inhibition to A-549 (human lung carcinoma) cancer cell lines with an IC50 value of 8.0 μM. |
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| Keywords: | Cholesterol B-norsteroid A-homosteroids A-homo-B-nor-steroidal derivatives Steroidal thiosemicarbazone |
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