title: Synthesis and antiproliferative activity of some steroidal thiosemicarbazones, semicarbazones and hydrozones.
abstract: Steroidal thiosemicarbazones, semicarbazones and hydrazones have received extensive attention of scientists recently because they exhibit some biological activities such as antibacterial, antiviral and anticancer. Using different steroids as starting materials, through different chemical methods, 24 steroidal compounds with thiosemicarbazone, semicarbazone or hydrazone groups in their structures, were synthesized, characterized by IR, NMR and MS. The antiproliferative activity of the compounds was evaluated against human gastric cancer (SGC-7901) and human liver cancer (Bel-7404) cells. The structure-activity relationship of these compounds was discussed. The results showed that compound 3 and 12a-12c exhibited significant inhibitory activity to Bel-7404 cells, and IC50 values of them were 4.2, 11.0, 7.4 and 15.0μM respectively (Cisplatin, IC50: 11.6μM).
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China.
authors.forename: Chunfang
authors.initials: C
authors.lastname: Gan
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China. Electronic address: cuijg1954@126.com.
authors.forename: Jianguo
authors.initials: J
authors.lastname: Cui
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China.
authors.forename: Shaoyang
authors.initials: S
authors.lastname: Su
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China.
authors.forename: Qifu
authors.initials: Q
authors.lastname: Lin
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China.
authors.forename: Linyi
authors.initials: L
authors.lastname: Jia
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China.
authors.forename: Lianghua
authors.initials: L
authors.lastname: Fan
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China. Electronic address: huangyanmin828@163.com.
authors.forename: Yanmin
authors.initials: Y
authors.lastname: Huang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D006801:Humans; D006835:Hydrazones / Q000737:chemistry*; D013256:Steroids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D006835:Hydrazones; D013256:Steroids; D013882:Thiosemicarbazones
keywords: Antiproliferative activity; Cholesterol; Steroidal semicarbazones; Steroidal thiosemicarbazones; Stigmasterol