title: Synthesis of 1-benzyl-3-(5-hydroxymethyl-2-furyl)selenolo[3,2-c]pyrazole derivatives as new anticancer agents.
abstract: As part of our continuing search for potential anticancer drug candidates among YC-1 analogs, 1, 3-disubstituted selenolo[3,2-c]pyrazole derivatives were synthesized and evaluated for their cytotoxicity against NCI-H226 non-small cell lung cancer and A-498 renal cancer cell lines. Significant cytotoxicity was observed in 3-(5-hydroxymethyl-2-furyl) derivatives (2, 33, 36 and 37). Among them, compound 2 was found to have the most potent activity. The mode of action of compound 2 seems to differ from those of the 175 anticancer agents listed in NCI's standard database and resembles that of YC-1. Thus, we recommend that compound 2 should be developed further as new drug candidate for treatment of non-small cell lung cancer and renal cancer.
authors.affiliation: Graduate Institute of Pharmaceutical Chemistry, China Medical University, 91 Shueh Shih Road, North Section, Taichung 40402, Taiwan.
authors.forename: Li-Chen
authors.initials: LC
authors.lastname: Chou
authors.forename: Li-Jiau
authors.initials: LJ
authors.lastname: Huang
authors.forename: Mei-Hua
authors.initials: MH
authors.lastname: Hsu
authors.forename: Mei-Chi
authors.initials: MC
authors.lastname: Fang
authors.forename: Jai-Sing
authors.initials: JS
authors.lastname: Yang
authors.forename: Shi-Hong
authors.initials: SH
authors.lastname: Zhuang
authors.forename: Hui-Yi
authors.initials: HY
authors.lastname: Lin
authors.forename: Fang-Yu
authors.initials: FY
authors.lastname: Lee
authors.forename: Che-Ming
authors.initials: CM
authors.lastname: Teng
authors.forename: Sheng-Chu
authors.initials: SC
authors.lastname: Kuo
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared
chemical_list: D000970:Antineoplastic Agents; D011720:Pyrazoles