- Design and synthesis of novel 2,4-diaryl-5H-indeno[1,2-b]pyridine derivatives, and their evaluation of topoisomerase inhibitory activity and cytotoxicity
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For the development of potential anticancer agents, we designed and synthesized 30 new 2,4-diaryl-5H-indeno[1,2-b]pyridine derivatives containing aryl moiety such as furyl, thienyl, pyridyl, and phenyl at 2- and 4-position of 5H-indeno[1,2-b]pyridine. The
- Kadayat, Tara Man,Park, Chanmi,Jun, Kyu-Yeon,Magar, Til Bahadur Thapa,Bist, Ganesh,Yoo, Han Young,Kwon, Youngjoo,Lee, Eung-Seok
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- Novel 2-aryl-4-(4′-hydroxyphenyl)-5H-indeno[1,2-b]pyridines as potent DNA non-intercalative topoisomerase catalytic inhibitors
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On the basis of previous reports on the importance of thienyl, furyl or phenol group substitution on 5H-indeno[1,2-b]pyridine skeleton, a new series of rigid 2-aryl-4-(4′-hydroxyphenyl)-5H-indeno[1,2-b]pyridine derivatives were systematically designed and
- Park, Seojeong,Kadayat, Tara Man,Jun, Kyu-Yeon,Thapa Magar, Til Bahadur,Bist, Ganesh,Shrestha, Aarajana,Lee, Eung-Seok,Kwon, Youngjoo
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- Co(II) and Mn(II) coordination polymers: Ligand functional and positional isomeric effects, structural diversities, luminescence sensing and magnetic properties
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Two new isostructural 3D Co(II) and Mn(II) coordination polymers (CPs) [M(L1′)2] (M = Co(1) and Mn (2)) were prepared by reactions of metal salts and 2-connected 4-(4-(3-cyanophenyl)-[2,3′-bipyridin]-6-yl)benzoic acid ligand (HL1′). Interestingly, when simple modification of the ligand functional group (from the cyano to carboxylate group), other two new 3D Co(II) [Co(HL2′)2] (3) and Mn(II) [Mn(L2′)(H2O)] (4) CPs are constructed by using 3-connected 3-(6-(4-carboxyphenyl)-[2,3′-bipyridin]-4-yl) benzoic acid (H2L2′), which are ascribed to the change in ligand functionality (from the cyano to carboxylate group). Moreover, the variable positions of cyano group (or carboxylate group) at the ligand isomers also can tune structural diversities. Present and previous works indicate that the isomeric effects of the ligand isomers play important role in adjusting structures of the Co(II) CPs. 1–4 were fully characterized by IR, elemental analyses, TGA, PXRD, and single-crystal X-ray diffraction. Interestingly, 2 and 4 can serve as sensing materials for detecting Fe3+ and Cr2O72? ions. Furthermore, the magnetic properties of four CPs have been investigated. The present work provides a promising approach to design and construct CPs or MOFs by adjusting ligand functionality and positional isomeric effects.
- Yan, Qing-Qing,Li, Bin,Yong, Guo-Ping
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- Crystal structures and properties of four coordination polymers based on a new asymmetric ligand: Tuning structure/dimensionality by various organic solvents
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An asymmetric ligand, 4,4′-([2,3′-bipyridine]-4,6-diyl)dibenzoic acid (H2L) was successfully used to construct four new coordination polymers, namely [M(HL)2]n (M = Cd(1), Co(2), Zn(3)) and [Ni(L)(H2O)2/su
- Li, Bin,Yan, Qing-Qing,Yong, Guo-Ping
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- Synthesis and biological activity of 2,4-di-p-phenolyl-6-2-furanyl-pyridine as a potent topoisomerase II poison
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Dihydroxylated 2,4-diphenyl-6-aryl pyridine derivatives were simply achieved using Claisen-Schmidt condensation reaction and modified Kr?hnke pyridine synthetic method. Total forty-five compounds were designed and synthesized which contain hydroxyl groups
- Karki, Radha,Park, Chanmi,Jun, Kyu-Yeon,Kadayat, Tara Man,Lee, Eung-Seok,Kwon, Youngjoo
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p. 360 - 378
(2015/03/18)
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- Synthesis and biological activity of 2,4-di- p -phenolyl-6- 2 -furanyl-pyridine as a potent topoisomerase II poison
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Dihydroxylated 2,4-diphenyl-6-aryl pyridine derivatives were simply achieved using Claisen-Schmidt condensation reaction and modified Kr?hnke pyridine synthetic method. Total forty-five compounds were designed and synthesized which contain hydroxyl groups
- Karki, Radha,Park, Chanmi,Jun, Kyu-Yeon,Kadayat, Tara Man,Lee, Eung-Seok,Kwon, Youngjoo
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p. 360 - 378
(2015/02/19)
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- 2,4-Diaryl-5,6-dihydro-1,10-phenanthroline and 2,4-diaryl-5,6- dihydrothieno[2,3-h] quinoline derivatives for topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study
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Designed and synthesized thirty-two 2,4-diaryl-5,6-dihydro-1,10- phenanthroline and 2,4-diaryl-5,6-dihydrothieno[2,3-h] quinoline derivatives as rigid analogs of 2,4,6-trisubstituted pyridines were evaluated for topoisomerase I and II inhibitory activitie
- Thapa, Pritam,Karki, Radha,Yoo, Han Young,Park, Pil-Hoon,Lee, Eunyoung,Jeon, Kyung-Hwa,Na, Younghwa,Cho, Won-Jea,Kwon, Youngjoo,Lee, Eung-Seok
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experimental part
p. 67 - 78
(2012/04/10)
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- Design, synthesis, and antitumor evaluation of 2,4,6-triaryl pyridines containing chlorophenyl and phenolic moiety
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We have designed and synthesized a series of 2,4,6-triaryl pyridine derivatives containing chlorophenyl and phenolic moeity at 2- and 4- position of the central pyridine, respectively, resulting in a total of 42 compounds. They were evaluated for topoisom
- Thapa, Pritam,Karki, Radha,Yun, Minho,Kadayat, Tara Man,Lee, Eunyoung,Kwon, Han Byeol,Na, Younghwa,Cho, Won-Jea,Kim, Nam Doo,Jeong, Byeong-Seon,Kwon, Youngjoo,Lee, Eung-Seok
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experimental part
p. 123 - 136
(2012/07/27)
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- Synthesis of 2,4,6-tripyridyl pyridines, and evaluation of their antitumor cytotoxicity, topoisomerase i and II inhibitory activity, and structure-activity relationship
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A series of 2,4,6-tripyridyl pyridines were synthesized, and evaluated for their antitumor cytotoxicity, topoisomerase I and II inhibitory activity. From the eighteen prepared compounds, compounds 10-12 have shown better or similar cytotoxicity against several human cancer cell lines as compared to 2,2':6',2''- terpyridine and doxorubicin. Especially, compound 10 exhibited the most potent cytotoxicity better than positive controls. Structure-activity relationship study indicated that 2,2':6',2''-terpyridine skeleton has an important role in displaying significant cytotoxicity against several human cancer cell lines.
- Jeong, Byeong-Seon,Choi, Hoyoung,Kwak, Young-Shin,Lee, Eung-Seok
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experimental part
p. 3566 - 3570
(2012/01/11)
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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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- 2-Thienyl-4-furyl-6-aryl pyridine derivatives: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study
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Designed and synthesized 60 2-thienyl-4-furyl-6-aryl pyridine derivatives were evaluated for their topoisomerase I and II inhibitory activities at 20 μM and 100 μM and cytotoxicity against several human cancer cell lines. Compounds 8, 9, 11-29 showed sign
- Thapa, Pritam,Karki, Radha,Thapa, Uttam,Jahng, Yurngdong,Jung, Mi-Ja,Nam, Jung Min,Na, Younghwa,Kwon, Youngjoo,Lee, Eung-Seok
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experimental part
p. 377 - 386
(2010/04/02)
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- Synthesis of 2-(thienyl-2-yl or -3-yl)-4-furyl-6-aryl pyridine derivatives and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship
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A series of 2-(thienyl-2-yl or -3-yl)-4-furyl-6-aryl pyridine derivatives were designed, synthesized, and evaluated for their topoisomerase I and II inhibition and cytotoxic activity against several human cancer cell lines. Compounds 10-19 showed moderate
- Thapa, Pritam,Karki, Radha,Choi, Hoyoung,Choi, Jae Hun,Yun, Minho,Jeong, Byeong-Seon,Jung, Mi-Ja,Nam, Jung Min,Na, Younghwa,Cho, Won-Jea,Kwon, Youngjoo,Lee, Eung-Seok
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experimental part
p. 2245 - 2254
(2010/06/14)
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- Synthesis of 2,6-diaryl-substituted pyridines and their antitumor activities
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For the development of novel antitumor agents, we designed and synthesized 2,6-diaryl-substituted pyridine derivatives bearing three aryl groups, which are the bioisosteres of terpyridine, and evaluated their biological activities. Most of the 18 prepared compounds showed moderate cytotoxicity against several human cancer cell lines. From the structure-activity relationships we may conclude that the number of aryl groups employed would be critical for their biological activities.
- Son, Jong-Keun,Zhao, Long-Xuan,Basnet, Arjun,Thapa, Pritam,Karki, Radha,Na, Younghwa,Jahng, Yurngdong,Jeong, Tae Cheon,Jeong, Byeong-Seon,Lee, Chong-Soon,Lee, Eung-Seok
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p. 675 - 682
(2008/09/20)
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- 2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship
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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.
- 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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p. 4351 - 4359
(2008/03/12)
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