title: Synthesis and cytotoxic activity of some novel steroidal C-17 pyrazolinyl derivatives.
abstract: Fourteen novel steroidal C-17 pyrazolinyl derivatives 9a-g and 10a-g were synthesized from commercially available progesterone and tested for their cytotoxic activity against brine shrimp (Artemia salina) and three human cancer cell lines (NCI-H460, HeLa, and HepG2). Some of these synthetic compounds exhibited significant cytotoxic activity, and treatment of HeLa cells with compound 10b resulted in the cell population arrest in the S phase. A structure-activity relationship was discussed.
authors.affiliation: Shaanxi Engineering Center of Bioresource Chemistry & Sustainable Utilization, College of Science, Northwest A&F University, Yangling, Shaanxi 712100, China.
authors.forename: Ning-Juan
authors.initials: NJ
authors.lastname: Fan
authors.forename: Jiang-Jiang
authors.initials: JJ
authors.lastname: Tang
authors.forename: He
authors.initials: H
authors.lastname: Li
authors.forename: Xiao-Jun
authors.initials: XJ
authors.lastname: Li
authors.forename: Bo
authors.initials: B
authors.lastname: Luo
authors.forename: Jin-Ming
authors.initials: JM
authors.lastname: Gao
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D001156:Artemia / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D011720:Pyrazoles
keywords: Cytotoxicity; Progesterone; Pyrazoline; Steroid; Steroidal heterocycles