- Design, synthesis, biological evaluation, structure-activity relationship study, and mode of action of 2-phenol-4,6-dichlorophenyl-pyridines
-
Human DNA topoisomerases (Topos) are essential nuclear enzyme whose level of expression is potential indicator for prediction of responsive result of chemotherapy. Topos has become a key cellular target for most of the anticancer agents that regulates top
- Shrestha, Aarajana,Park, Seojeong,Shin, Somin,Man Kadayat, Tara,Bist, Ganesh,Katila, Pramila,Kwon, Youngjoo,Lee, Eung-Seok
-
-
Read Online
- 2-Chlorophenyl-substituted benzofuro[3,2-b]pyridines with enhanced topoisomerase inhibitory activity: The role of the chlorine substituent
-
A new series of 2-chloropheny-substituted benzofuro[3,2-b]pyridines were designed, synthesized, and evaluated for topoisomerase I and II inhibition and antiproliferative activity. Compounds 17–19, 23, 24, 26, and 27 exhibited excellent topo II inhibitory
- Thapa Magar, Til Bahadur,Kadayat, Tara Man,Lee, Hwa-Jong,Park, Seojeong,Bist, Ganesh,Shrestha, Aarajana,Kwon, Youngjoo,Lee, Eung-Seok
-
-
Read Online
- Stereoselective Synthesis of Atropisomeric Bipyridine N,N′-Dioxides by Oxidative Coupling
-
Bipyridine N,N′-dioxide is a structural fragment found in many bioactive compounds. Furthermore, chiral analogues secured their place as powerful Lewis base catalysts. The scope of the existing methods for the synthesis of atropisomeric bipyridine N,N′-di
- Fukazawa, Yasuaki,Vaganov, Vladimir Yu.,Shipilovskikh, Sergei A.,Rubtsov, Aleksandr E.,Malkov, Andrei V.
-
-
Read Online
- Kr?hnke pyridines: Rapid and facile access to Mcl-1 inhibitors
-
The tumorigenic activity of upregulated Mcl-1 is manifested by binding the BH3 α-helical death domains of opposing Bcl-2 family members, neutralizing them and preventing apoptosis. Accordingly, the development of Mcl-1 inhibitors largely focuses on synthe
- Conlon, Ivie L.,Van Eker, Daniel,Abdelmalak, Sameh,Murphy, William A.,Bashir, Hassan,Sun, Michael,Chauhan, Jay,Varney, Kristen M.,Godoy-Ruiz, Raquel,Wilder, Paul T.,Fletcher, Steven
-
-
Read Online
- 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
-
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
-
-
Read Online
- Cyclization of Active Methylene Isocyanides with α-Oxodithioesters Induced by Base: An Expedient Synthesis of 4-Methylthio/Ethoxycarbonyl-5-acylthiazoles
-
Cyclization of tosylmethyl isocyanide with α-oxodithioesters in the presence of KOH is reported for the synthesis of 4-methylthio-5-acylthiazoles. Similarly, ethyl isocyanoacetate underwent cyclization with α-oxodithioesters to form 4-ethoxycarbonyl-5-acy
- Anil, Seegehalli M.,Kiran, Kuppalli R.,Rajeev, Narasimhamurthy,Rangappa, Kanchugarakoppal S.,Sadashiva, Maralinganadoddi P.,Swaroop, Toreshettahally R.
-
p. 1444 - 1450
(2020/04/27)
-
- Optimization of Catalyst Structure for Asymmetric Propargylation of Aldehydes with Allenyltrichlorosilane
-
The design of catalysts for asymmetric propargylations remains a challenging task, with only a handful of methods providing access to enantioenriched homopropargylic alcohols. In this work, guided by previously reported computational predictions, a set of
- Vaganov, Vladimir Yu.,Fukazawa, Yasuaki,Kondratyev, Nikolay S.,Shipilovskikh, Sergei A.,Wheeler, Steven E.,Rubtsov, Aleksandr E.,Malkov, Andrei V.
-
p. 5467 - 5474
(2020/10/19)
-
- Acid-Catalyzed Condensation of o-Phenylenediammines and o-Aminophenols with α-Oxodithioesters: A Divergent and Regio? selective Synthesis of 2-Methylthio-3-Aryl/Heteroarylquinoxalines and 2-Acylbenzoxazoles
-
o-Phenylenediammines and o-Aminophenols were reacted with α-oxodithioesters in a highly regioselective fashion to give 2-methylthio-3-Aryl/heteroarylquinoxalines and 2-Acylbenzoxazoles in 55-94percent and 45-86percent, respectively, in the presence of p-T
- Anil, Seegehally M,Kiran, Kuppalli R,Rangappa, Kanchugarakoppal S,Sadashiva, Maralinganadoddi P,Shruthi, Jeegundipattana B,Sukrutha, Kodipura P,Swaroop, Toreshettahally R
-
p. 4205 - 4214
(2019/11/14)
-
- 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
-
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
-
p. 1909 - 1919
(2018/03/07)
-
- A new series of 2-phenol-4-aryl-6-chlorophenyl pyridine derivatives as dual topoisomerase I/II inhibitors: Synthesis, biological evaluation and 3D-QSAR study
-
As a continuous effort to develop novel antitumor agents, a new series of forty-five 2-phenol-4-aryl-6-chlorophenyl pyridine compounds were synthesized and evaluated for cytotoxicity against four different human cancer cell lines (DU145, HCT15, T47D, and HeLa), and topoisomerase I and II inhibitory activity. Several compounds (10-15, 20, 22, 24, 28, 42, and 49) displayed strong to moderate dual topoisomerase I and II inhibitory activity at 100 μM. It was observed that hydroxyl and chlorine moiety at meta or para position of phenyl ring is favorable for dual topoisomerase inhibitory activity and cytotoxicity. Most of the compounds displayed stronger cytotoxicities than those of all positive controls against the HCT15 and T47D cell lines. For investigation of the structure-activity relationships, a 3D-QSAR analysis using the method of comparative molecular field analysis (CoMFA) was performed. The generated 3D contour maps can be used for further rational design of novel terpyridine derivatives as highly selective and potent cytotoxic agents.
- Karki, Radha,Jun, Kyu-Yeon,Kadayat, Tara Man,Shin, Somin,Thapa Magar, Til Bahadur,Bist, Ganesh,Shrestha, Aarajana,Na, Younghwa,Kwon, Youngjoo,Lee, Eung-Seok
-
p. 228 - 245
(2016/03/08)
-
- Effect of chlorine substituent on cytotoxic activities: Design and synthesis of systematically modified 2,4-diphenyl-5H-indeno[1,2-b]pyridines
-
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
-
p. 1726 - 1731
(2016/07/27)
-
- 2-Thienyl-4-furyl-6-aryl pyridine derivatives: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study
-
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
-
experimental part
p. 377 - 386
(2010/04/02)
-
- 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
-
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
-
experimental part
p. 2245 - 2254
(2010/06/14)
-
- SYNTHESIS AND STRUCTURAL STUDY ON Α-SUBSTITUED-1-STYRYLPYRIDINIUM SALTS. REINVESTIGATION OF KROHNKE CONDENSATION
-
Kroehnke condensation of several cycloimmonium salts with p-dimethylaminobenzaldehyde has been studied.X-Ray diffraction, IR and Raman spectra, 1H- and 13C-NMR and UV spectra of the products are discussed, being compared, when necessary, with the starting pyridinium salts.All compounds showed the Z configuration, corresponding to the more stable structure, except one, in which steric factors were predominant.
- Alvarez-Builla, J.,Novella, J. L.,Galvez, E.,Smith, P.,Florencio, F.,et al.
-
p. 699 - 708
(2007/10/02)
-