- A B2(OH)4-Mediated Synthesis of 2-Substituted Indazolone and Its Application in a DNA-Encoded Library
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Indazolone cores are among the most common structural components in medicinal chemistry and can be found in many biologically active molecules. In this report, a mild and efficient approach to 2-substituted indazolones via B2(OH)4-mediated reductive N-N b
- Bao, Yapeng,Deng, Zongfa,Feng, Jing,Zhu, Weiwei,Li, Jin,Wan, Jinqiao,Liu, Guansai
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supporting information
p. 6277 - 6282
(2020/08/24)
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- Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: Discovery of CCKR1 selectivity in a previously CCKR2-selective lead series
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A series of CCK2R-selective anthranilic amides is shown to derive CCK1R affinity via selective substitution of the amide side chain. Thus, extending the length of the original benzamide side chain by a single methylene unit imparts CCK1R affinity to the s
- Pippel, Marna,Allison, Brett D.,Phuong, Victor K.,Li, Lina,Morton, Magda F.,Prendergast, Clodagh,Wu, Xiaodong,Shankley, Nigel P.,Rabinowitz, Michael H.
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scheme or table
p. 6373 - 6375
(2010/04/30)
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- Synthesis and?antitumor activity of?cis-dichloroplatinum(II) complexes of?1-(2-aminophenyl)-1,2,3,4-tetrahydroisoquinolines
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Fifteen cis-dichloroplatinum complexes (5a-5o) were synthesized by treatment of 1-(2-aminophenyl)-1,2,3,4-THIQs (4a-4o) with K2PtCl4. The antitumor activity of these compounds was examined against four different human tumor cell lines. Their structure-activity relationships for antitumor activity are reported. All of these compounds exhibited activity against MCF-7 cell line and showed good activity against WiDr cell line except 5c and 5f. On the other hand, compounds 5j and 5o are more active than the other compounds against Hepa59T/VGH cell line. The electron-donating group at the 6-position of isoquinoline ring seems to decrease the antitumor activity and the chloro substituent at the C-4 position of the aniline ring shown the highest potency. The "trans influence" dominates the control of the stability of [1-(2-aminophenyl)-1,2,3,4-THIQ]dichloroplatinums(II).
- Kuo, Chen-Yuan,Wu, Ming-Jung,Kuo, Yao-Haur
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p. 940 - 949
(2007/10/03)
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