Synthesis of 1-benzyl-3-(5-hydroxymethyl-2-furyl)selenolo[3,2-c]pyrazole derivatives as new anticancer agents.
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.
Chou
Li-Chen
LC
Graduate Institute of Pharmaceutical Chemistry, China Medical University, 91 Shueh Shih Road, North Section, Taichung 40402, Taiwan.
Huang
Li-Jiau
LJ
Hsu
Mei-Hua
MH
Fang
Mei-Chi
MC
Yang
Jai-Sing
JS
Zhuang
Shi-Hong
SH
Lin
Hui-Yi
HY
Lee
Fang-Yu
FY
Teng
Che-Ming
CM
Kuo
Sheng-Chu
SC
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
D000970:Antineoplastic Agents; D011720:Pyrazoles