- Design, synthesis, and structure-activity relationships of new benzofuro[3,2-b]pyridin-7-ols as DNA topoisomerase II inhibitors
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Human DNA topoisomerases have become attractive targets for developing more effective anticancer drugs. In this study, a series of new benzofuro[3,2-b]pyridin-7-ols were designed and synthesized for the first time and screened for their topoisomerase I and II inhibitory and antiproliferative activity. Structure-activity relationships revealed the position of ortho- and para-hydroxyl group at 2-phenyl ring, and meta-hydroxyl group at 4-phenyl ring of benzofuro[3,2-b]pyridin-7-ol are important for potent and selective topo II inhibitory activity. Compound 11 showed the most selective and potent topo II inhibition (100% inhibition at 100 μM) and strongest antiproliferative activity (IC50 = 0.86 μM) than all the positive controls in HeLa cell line.
- Shrestha, Aarajana,Jo, Hyunji,Kwon, Youngjoo,Lee, Eung-Seok
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p. 566 - 571
(2018/02/09)
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- Synthesis and SAR study of new hydroxy and chloro-substituted 2,4-diphenyl 5H-chromeno[4,3-b]pyridines as selective topoisomerase IIα-targeting anticancer agents
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As part of our effort to develop potential topoisomerase IIα (topo IIα) targeting anticancer agents, we systematically designed a new series of hydroxy and chloro-substituted 2,4-diphenyl 5H-chromeno[4,3-b]pyridines. Total eighteen compounds were synthesi
- Magar, Til Bahadur Thapa,Seo, Seung Hee,Kadayat, Tara Man,Jo, Hyunji,Shrestha, Aarajana,Bist, Ganesh,Katila, Pramila,Kwon, Youngjoo,Lee, Eung-Seok
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p. 1909 - 1919
(2018/03/07)
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- Dihydroxylated 2,6-diphenyl-4-chlorophenylpyridines: Topoisomerase I and IIα dual inhibitors with DNA non-intercalative catalytic activity
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With the aim to develop novel antiproliferative agents, a new series of eighteen dihydroxylated 2,6-diphenyl-4-chlorophenylpyridines were systematically designed, prepared, and investigated for their topoisomerase (topo) I and IIα inhibitory properties an
- Bist, Ganesh,Park, Seojeong,Song, Chanju,Thapa Magar, Til Bahadur,Shrestha, Aarajana,Kwon, Youngjoo,Lee, Eung-Seok
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- Rational design, synthesis, and evaluation of novel 2,4-Chloro- and Hydroxy-Substituted diphenyl Benzofuro[3,2-b]Pyridines: Non-intercalative catalytic topoisomerase I and II dual inhibitor
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Novel series of conformationally constrained 2,4-chloro- and hydroxy-substituted diphenyl benzofuro[3,2-b]pyridines were rationally designed and synthesized. Their biological activities were evaluated for topoisomerase I and II inhibitory activity, and an
- Park, Seojeong,Thapa Magar, Til Bahadur,Kadayat, Tara Man,Lee, Hwa Jong,Bist, Ganesh,Shrestha, Aarajana,Lee, Eung-Seok,Kwon, Youngjoo
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p. 318 - 333
(2017/01/10)
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- Effect of chlorine substituent on cytotoxic activities: Design and synthesis of systematically modified 2,4-diphenyl-5H-indeno[1,2-b]pyridines
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In continuation of our previous work, six hydroxylated 2,4-diphenyl-5H-indeno[1,2-b]pyridine analogs were modified by introducing one chlorine functionality at ortho, meta or para position of the 2- or 4-phenyl ring. Eighteen new chlorinated compounds wer
- Kadayat, Tara Man,Park, Seojeong,Jun, Kyu-Yeon,Magar, Til Bahadur Thapa,Bist, Ganesh,Shrestha, Aarajana,Na, Younghwa,Kwon, Youngjoo,Lee, Eung-Seok
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p. 1726 - 1731
(2016/07/27)
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- Topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of dihydroxylated 2,6-diphenyl-4-aryl pyridines
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Abstract A new series of thirty-six dihydroxylated 2,6-diphenyl-4-aryl pyridines containing hydroxyl groups at the ortho, meta, or para position of 2- and 6-phenyl rings attached to the central pyridine were designed and synthesized. They were evaluated f
- Karki, Radha,Song, Chanju,Kadayat, Tara Man,Magar, Til Bahadur Thapa,Bist, Ganesh,Shrestha, Aarajana,Na, Younghwa,Kwon, Youngjoo,Lee, Eung-Seok
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p. 3638 - 3654
(2015/08/03)
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- A series of novel terpyridine-skeleton molecule derivants inhibit tumor growth and metastasis by targeting topoisomerases
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A series of novel terpyridine-skeleton molecules containing conformational rigidity, 14 containing benzo[4,5]furo[3,2-b]pyridine core and 15 comprising chromeno[4,3-b]pyridine core, were synthesized, and their biological activities were evaluated. 3-(4-Ph
- Kwon, Han-Byeol,Park, Chanmi,Jeon, Kyung-Hwa,Lee, Eunyoung,Park, So-Eun,Jun, Kyu-Yeon,Kadayat, Tara Man,Thapa, Pritam,Karki, Radha,Na, Younghwa,Park, Mi Sun,Rho, Seung Bae,Lee, Eung-Seok,Kwon, Youngjoo
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p. 1100 - 1122
(2015/03/04)
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- Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of 2-phenyl- or hydroxylated 2-phenyl-4-aryl-5H-indeno[1,2-b]pyridines
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Abstract A series of novel twenty-eight rigid 2-phenyl- or hydroxylated 2-phenyl-4-aryl-5H-indeno[1,2-b]pyridines were synthesized and evaluated for their topoisomerase inhibitory activity as well as their cytotoxicity against several human cancer cell li
- Kadayat, Tara Man,Song, Chanju,Shin, Somin,Magar, Til Bahadur Thapa,Bist, Ganesh,Shrestha, Aarajana,Thapa, Pritam,Na, Younghwa,Kwon, Youngjoo,Lee, Eung-Seok
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p. 3499 - 3512
(2015/08/03)
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- Design and synthesis of conformationally constrained hydroxylated 4-phenyl-2-aryl chromenopyridines as novel and selective topoisomerase II-targeted antiproliferative agents
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To develop novel selective topoisomerase II inhibitors, we designed and synthesized a series of conformationally constrained hydroxylated 4-phenyl-2-aryl chromenopyridines and evaluated their topoisomerase inhibitory activity and cytotoxicity against thre
- Thapa, Pritam,Jun, Kyu-Yeon,Kadayat, Tara Man,Park, Chanmi,Zheng, Zhi,Thapa Magar, Til Bahadur,Bist, Ganesh,Shrestha, Aarajana,Na, Younghwa,Kwon, Youngjoo,Lee, Eung-Seok
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p. 6454 - 6466
(2015/10/05)
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- Modified 2,4-diaryl-5H-indeno[1,2-b]pyridines with hydroxyl and chlorine moiety: Synthesis, anticancer activity, and structure-activity relationship study
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As a part of ongoing studies in developing novel anticancer agents, a series of modified 2,4-diaryl-5H-indeno[1,2-b]pyridines were designed, and synthesized by introducing hydroxyl and chlorine moieties. They were evaluated for topoisomerase inhibitory ac
- Kadayat, Tara Man,Song, Chanju,Kwon, Youngjoo,Lee, Eung-Seok
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- Dihydroxylated 2,4,6-triphenyl pyridines: Synthesis, topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study
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Twelve dihydroxylated 2,4,6-triphenyl pyridines were designed and synthesized which contain hydroxyl groups at ortho, meta or para position of 2- and 6-phenyl, or 2- and 4-phenyl rings attached to the central pyridine. They were evaluated for topoisomeras
- Karki, Radha,Thapa, Pritam,Yoo, Han Young,Kadayat, Tara Man,Park, Pil-Hoon,Na, Youngwha,Lee, Eunyoung,Jeon, Kyung-Hwa,Cho, Won-Jea,Choi, Heesung,Kwon, Youngjoo,Lee, Eung-Seok
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experimental part
p. 219 - 228
(2012/05/05)
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- Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines
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A new series of 2,4-diphenyl-6-aryl pyridines containing hydroxyl group(s) at the ortho, meta, or para position of the phenyl ring were synthesized, and evaluated for topoisomerase I and II inhibitory activity and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Structure-activity relationship study revealed that the substitution of hydroxyl group(s) increased topoisomerase I and II inhibitory activity in the order of meta > para > ortho position. Substitution of hydroxyl group on the para position showed better cytotoxicity.
- Karki, Radha,Thapa, Pritam,Kang, Mi Jeong,Jeong, Tae Cheon,Nam, Jung Min,Kim, Hye-Lin,Na, Younghwa,Cho, Won-Jea,Kwon, Youngjoo,Lee, Eung-Seok
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experimental part
p. 3066 - 3077
(2010/07/06)
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