2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship |
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Authors: | Basnet Arjun Thapa Pritam Karki Radha Na Younghwa Jahng Yurngdong Jeong Byeong-Seon Jeong Tae Cheon Lee Chong-Soon Lee Eung-Seok |
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Institution: | College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea. |
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Abstract: | Designed and synthesized were a series of pyridines substituted at 2, 4, and 6 positions with various 5- or 6-memberd heteroaromatics as antitumor agents. They were evaluated their topoisomerase I and II inhibitory activities along with cytotoxicities against several human cancer cell lines. Among the prepared compounds, 10-20 showed significant topoisomerase I or II inhibitory activities, and 21-26 showed considerable cytotoxicities against several human cancer cell lines. Structure-activity relationship study indicates that 4'-pyridine at 6-position of central pyridine plays a key role in biological activity. |
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