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Syntheses, Crystal Structures and Antitumor Activities of Two Nicotinamides

Syntheses, Crystal Structures and Antitumor Activities of Two Nicotinamides
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摘要 Two nicotinamides have been synthesized by coupling aromatic amines with equimolar quantities of substituted nicotinic acids. Their structures have been determined by X-ray single-crystal diffraction. Compound 1, 6-chloro-N-(4-fluorophenyl)nicotinamide, crystallizes in the triclinic space group Pī with a = 4.2188(8) , b = 5.0687(10), c = 25.956(5), α = 86.38(3), β = 87.75(3), γ = 83.20(3)°, V = 549.75(19) 3 and Z = 2. Compound 2, N-(quinolin-3-yl)nico- tinamide, crystallizes in the monoclinic space group P21 with a = 8.5100(17), b = 6.4230(13), c = 11.620(2) , β = 110.39(3)°, V = 595.3(2) 3 and Z = 2. The cytotoxic activities of the two nicotinamides against five human tumor cell lines were tested in vitro. The results indicated that they showed a wide range of antitumor activities. Two nicotinamides have been synthesized by coupling aromatic amines with equimolar quantities of substituted nicotinic acids. Their structures have been determined by X-ray single-crystal diffraction. Compound 1, 6-chloro-N-(4-fluorophenyl)nicotinamide, crystallizes in the triclinic space group Pī with a = 4.2188(8) , b = 5.0687(10), c = 25.956(5), α = 86.38(3), β = 87.75(3), γ = 83.20(3)°, V = 549.75(19) 3 and Z = 2. Compound 2, N-(quinolin-3-yl)nico- tinamide, crystallizes in the monoclinic space group P21 with a = 8.5100(17), b = 6.4230(13), c = 11.620(2) , β = 110.39(3)°, V = 595.3(2) 3 and Z = 2. The cytotoxic activities of the two nicotinamides against five human tumor cell lines were tested in vitro. The results indicated that they showed a wide range of antitumor activities.
出处 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2013年第5期631-636,共6页 结构化学(英文)
基金 supported by the National Natural Science Foundation of China (No. 21102182) the Research Fund of young scholars for the Doctoral Program of Higher Education of China (No. 20110096120008)
关键词 SYNTHESIS crystal structure ANTITUMOR NICOTINAMIDE synthesis, crystal structure, antitumor, nicotinamide
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  • 1Stratigos, J. D.; Katsambas, A. Pellagra: a still existing disease. Br. J. Dermatol. 1977, 96, 99-106. 被引量:1
  • 2Altschul, R.; Hoffer, A.; Stephen, J. D. Influence of nicotinic acid on serum cholesterol in man. Arch. giochem 1955, 54, 558-559. 被引量:1
  • 3Carlson, L. A. Nicotinic acid: the broad-spectrum lipid drug. A 50th anniversary review..Z lntern. Med. 2005, 258, 94--114. 被引量:1
  • 4Offermalms, S. The nicotinic acid receptor GPR109A (HM74A or PUMA-G) as a new therapeutic target. Trends Pharmacol. Sci. 2006, 27, 384-390. 被引量:1
  • 5Canner, P. L.; Berge, K. G; Wenger, N. K.; Stamler, J.; Friedman, L.; Prineas, R. J.; Friedewald, W. Fifteen year mortality in Coronary Drug Project patients: long-term benefit with niacin. J. Am. Coll. Cardiol. 1986, 8, 1245-1255. 被引量:1
  • 6Berge, K. G; Canner, P. L. Coronary drug project: experience with niacin. Euv J. Clin. Pharmacol. 1991, 40, S49-S51. 被引量:1
  • 7Wendt, M. D.; Rockway, T. W.; Geyer, A.; McClellan, W.; Weitzberg, M.; Zhao, X.; Mantei, R.; Nienaber, V. L.; Stewart, K.; Klinghofer, V.; Giranda, V. L. Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR ofN-phenyl amide 6-substitution. J. Med. Chem. 2004, 47, 303-324. 被引量:1
  • 8Kakuta, H.; Zheng, X.; Oda, H.; Harada, S.; Sugimoto, Y.; Sasaki, K.; Tai, A. Cyclooxygenase-l-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. Design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor. J. Med. Chem. 2008, 51, 2400-2411. 被引量:1
  • 9Yang, Y.; Shi, L.; Zhou, Y.; Li, H. Q.; Zhu, Z. W.; Zhu, H. L. Design, synthesis and biological evaluation of quinoline amide derivatives as novel VEGFR-2 inhibitors. Bioorg. Med. Chem. Lett. 2010, 20, 6653-6656. 被引量:1
  • 10Shi, L.; Li, Z. L.; Yang, Y.; Zhu, Z. W.; Zhu, H. L. Design of novel N-phenylnicotinamides as selective cyclooxygenase-1 inhibitors. Bioorg. Med Chem. Lett. 2011, 21,121-124. 被引量:1

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