nach oben

Erschienen in:

2014 | OriginalPaper | Buchkapitel

93. Design, Synthesis and Primary Biological Evaluation of the Novel Antitumor Agent Indoline-3-One and Its Derivatives

verfasst von : Haiyong Jia, Guojun Pan, Yiqian Wang, Shaopeng Wen, Qiannan Guo, Weiguo Hu, Peng Yu, Hua Sun, Yuou Teng

Erschienen in: Proceedings of the 2012 International Conference on Applied Biotechnology (ICAB 2012)

Verlag: Springer Berlin Heidelberg

Einloggen

Aktivieren Sie unsere intelligente Suche, um passende Fachinhalte oder Patente zu finden.

search-config

KI-gestützte Suche

Aus

Abstract

Indolinone displays promising antitumor properties by inhibiting various kinase families. In this paper, we’d like to report the design, synthesis, and primary biological evaluation of the novel indoline-3-one and its derivatives. All the newly synthesized compounds including the novel compound 2-(4-(trifluoromethyl)benzylidene)indolin-3-one (5f) were characterized by ¹H NMR and their antitumor activities were evaluated by using MTT method in HT-29, K562, and HepG2 cell lines. 2-(2-nitrobenzylidene)indolin-3-one (5d) demonstrated good antitumor activity against HT-29, K562, and HepG2 with an IC₅₀ of 2.04 μM, 2.33 μM, 2.24 μM, respectively. 2-(4-(trifluoromethyl)benzylidene)indolin-3-one(5f) demonstrated good antitumor activity against K562 and HepG2 with an IC₅₀ of 2.27 μM, 3.47 μM.

Sie haben noch keine Lizenz? Dann Informieren Sie sich jetzt über unsere Produkte:

Springer Professional "Wirtschaft+Technik"

Online-Abonnement

Mit Springer Professional "Wirtschaft+Technik" erhalten Sie Zugriff auf:

über 102.000 Bücher
über 537 Zeitschriften

aus folgenden Fachgebieten:

Automobil + Motoren
Bauwesen + Immobilien
Business IT + Informatik
Elektrotechnik + Elektronik
Energie + Nachhaltigkeit
Finance + Banking
Management + Führung
Marketing + Vertrieb
Maschinenbau + Werkstoffe
Versicherung + Risiko

Jetzt Wissensvorsprung sichern!

Jetzt informieren

Springer Professional "Technik"

Online-Abonnement

Mit Springer Professional "Technik" erhalten Sie Zugriff auf:

über 67.000 Bücher
über 390 Zeitschriften

aus folgenden Fachgebieten:

Automobil + Motoren
Bauwesen + Immobilien
Business IT + Informatik
Elektrotechnik + Elektronik
Energie + Nachhaltigkeit
Maschinenbau + Werkstoffe

Jetzt Wissensvorsprung sichern!

Jetzt informieren

Vorheriges Kapitel Stigmasterol from the Flowers of Trollius chinensis

Nächstes Kapitel Research Progress on the Anti-Rheumatoid Arthritis Drugs

Prakash CR, Raja S (2012) Indolinones as promising scaffold as kinase inhibitors: a review. Mini Rev Med Chem. 12(2):98–119CrossRef

Krystal GW, Honsawek S, Kiewlich D et al (2001) Indolinone tyrosine kinase inhibitors block Kit activation and growth of small cell lung cancer cells. Cancer Res 61(9):3660–3668

Wood L (2012) Sunitinib malate for the treatment of renal cell carcinoma. Expert Opin Pharmacother 13(9):1323–1336CrossRef

Raymond E, Hammel P, Dreyer C et al (2012) Sunitinib in pancreatic neuroendocrine tumors. Target Oncol 7(2):117–125CrossRef

Naraev BG, Strosberg JR, Halfdanarson TR (2012) Current status and perspectives of targeted therapy in well-differentiated neuroendocrine tumors. Oncology 83(3):117–127CrossRef

Figlin R, Sternberg C, Wood CG (2012) Novel agents and approaches for advanced renal cell carcinoma. J Urol 188(3):707–715CrossRef

Ito T, Igarashi H, Jensen RT et al (2012) Current status and therapeutic strategy for pancreatic neuroendocrine tumors in Japan. Fukuoka Igaku Zasshi 103(7):131–137

Chen Z, Merta PJ, Lin NH et al (2005) A-432411, a novel indolinone compound that disrupts spindle pole formation and inhibits human cancer cell growth. Mol Cancer Ther 4(4):562–568CrossRef

Mulligan JM, Greene LM, Cloonan S et al (2006) Identification of tubulin as the molecular target of proapoptotic pyrrolo-1,5-benzoxazepines. Mol Pharmacol 70(1):60–70

10.

Halaban R (1991) Growth factors and tyrosine protein kinases in normal and malignant melanocytes. Cancer Metastasis Rev 10(2):129–140CrossRef

11.

Bishop JM (1987) The molecular genetics of cancer. Science 235(4786):305–311CrossRef

12.

Sun L, Tran N, Tang F et al (1998) Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases. J Med Chem 41(14):2588–2603CrossRef

13.

Lee CY, Chew EH, Go ML (2010) Functionalized aurones as inducers of NAD(P)H:quinone oxidoreductase 1 that activate AhR/XRE and Nrf2/ARE signaling pathways: synthesis, evaluation and SAR. Eur J Med Chem 45:2957–2971CrossRef

14.

Islam I, Bryant J, Chou YL et al (2004) Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett 17(14):3814–3818CrossRef

15.

Nirogi RV, Deshpande AD, Kambhampati R et al (2011) Indole-3-piperazinyl derivatives: novel chemical class of 5-HT(6) receptor antagonists. Bioorg Med Chem Lett 21(1):346–349CrossRef

16.

Zhang W, Go ML (2009) Functionalized 3-benzylidene-indolin-2-ones: inducers of NAD(P)H-quinone oxidoreductase 1 (NQO1) with antiproliferative activity. Bioorg Med Chem 17(5):2077–2090CrossRef

Titel: Design, Synthesis and Primary Biological Evaluation of the Novel Antitumor Agent Indoline-3-One and Its Derivatives
verfasst von: Haiyong Jia
Guojun Pan
Yiqian Wang
Shaopeng Wen
Qiannan Guo
Weiguo Hu
Peng Yu
Hua Sun
Yuou Teng
Verlag: Springer Berlin Heidelberg
Buch: Proceedings of the 2012 International Conference on Applied Biotechnology (ICAB 2012)
Print ISBN: 978-3-642-37921-5

Electronic ISBN: 978-3-642-37922-2

Copyright-Jahr: 2014
DOI: https://doi.org/10.1007/978-3-642-37922-2_93

Premium Partner

Marktübersichten

Die im Laufe eines Jahres in der „adhäsion“ veröffentlichten Marktübersichten helfen Anwendern verschiedenster Branchen, sich einen gezielten Überblick über Lieferantenangebote zu verschaffen.

Zur Marktübersicht