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Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors.

Lin NH, Xia P, Kovar P, Park C, Chen Z, Zhang H, Rosenberg SH, Sham HL
Bioorg Med Chem Lett 16 421-6 (2006)
Cited: 13 times
EuropePMC logo PMID: 16242328

Abstract

Chk1 inhibitors have emerged as a novel class of neoplastic agents for abrogating the G2 DNA damage checkpoint arrest. Analogs of the Chk1 inhibitor, 3-ethylidene-1,3-dihydro-indol-2-one, were synthesized and tested in vitro for their inhibitory activities. The most promising compound identified from this series is analog 28, which possesses potent enzymatic and cellular activities.

Articles - 2ayp mentioned but not cited (2)

  1. Classifying kinase conformations using a machine learning approach. McSkimming DI, Rasheed K, Kannan N. BMC Bioinformatics 18 86 (2017)
  2. Discovery of novel checkpoint kinase 1 inhibitors by virtual screening based on multiple crystal structures. Li Y, Kim DJ, Ma W, Lubet RA, Bode AM, Dong Z. J Chem Inf Model 51 2904-2914 (2011)


Articles citing this publication (11)

  1. CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs. Walton MI, Eve PD, Hayes A, Valenti MR, De Haven Brandon AK, Box G, Hallsworth A, Smith EL, Boxall KJ, Lainchbury M, Matthews TP, Jamin Y, Robinson SP, Aherne GW, Reader JC, Chesler L, Raynaud FI, Eccles SA, Collins I, Garrett MD. Clin Cancer Res 18 5650-5661 (2012)
  2. 4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors. Ni ZJ, Barsanti P, Brammeier N, Diebes A, Poon DJ, Ng S, Pecchi S, Pfister K, Renhowe PA, Ramurthy S, Wagman AS, Bussiere DE, Le V, Zhou Y, Jansen JM, Ma S, Gesner TG. Bioorg Med Chem Lett 16 3121-3124 (2006)
  3. A myosin V inhibitor based on privileged chemical scaffolds. Islam K, Chin HF, Olivares AO, Saunders LP, De La Cruz EM, Kapoor TM. Angew Chem Int Ed Engl 49 8484-8488 (2010)
  4. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Islam I, Bryant J, Chou YL, Kochanny MJ, Lee W, Phillips GB, Yu H, Adler M, Whitlow M, Ho E, Lentz D, Polokoff MA, Subramanyam B, Wu JM, Zhu D, Feldman RI, Arnaiz DO. Bioorg Med Chem Lett 17 3814-3818 (2007)
  5. Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors. Tong Y, Claiborne A, Stewart KD, Park C, Kovar P, Chen Z, Credo RB, Gu WZ, Gwaltney SL, Judge RA, Zhang H, Rosenberg SH, Sham HL, Sowin TJ, Lin NH. Bioorg Med Chem 15 2759-2767 (2007)
  6. Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors. Huang S, Garbaccio RM, Fraley ME, Steen J, Kreatsoulas C, Hartman G, Stirdivant S, Drakas B, Rickert K, Walsh E, Hamilton K, Buser CA, Hardwick J, Mao X, Abrams M, Beck S, Tao W, Lobell R, Sepp-Lorenzino L, Yan Y, Ikuta M, Murphy JZ, Sardana V, Munshi S, Kuo L, Reilly M, Mahan E. Bioorg Med Chem Lett 16 5907-5912 (2006)
  7. Structure-based and shape-complemented pharmacophore modeling for the discovery of novel checkpoint kinase 1 inhibitors. Chen XM, Lu T, Lu S, Li HF, Yuan HL, Ran T, Liu HC, Chen YD. J Mol Model 16 1195-1204 (2010)
  8. Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis. Zhong Y, Xue M, Zhao X, Yuan J, Liu X, Huang J, Zhao Z, Li H, Xu Y. Bioorg Med Chem 21 1724-1734 (2013)
  9. Synthesis and biological evaluation of 4'-(6,7-disubstituted-2,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-biphenyl-4-ol as potent Chk1 inhibitors. Tao ZF, Li G, Tong Y, Chen Z, Merta P, Kovar P, Zhang H, Rosenberg SH, Sham HL, Sowin TJ, Lin NH. Bioorg Med Chem Lett 17 4308-4315 (2007)
  10. Discovery of 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2'-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors. Tao ZF, Li G, Tong Y, Stewart KD, Chen Z, Bui MH, Merta P, Park C, Kovar P, Zhang H, Sham HL, Rosenberg SH, Sowin TJ, Lin NH. Bioorg Med Chem Lett 17 5944-5951 (2007)
  11. Computational studies on the binding mechanism between triazolone inhibitors and Chk1 by molecular docking and molecular dynamics. Lv M, Ma S, Tian Y, Zhang X, Lv W, Zhai H. Mol Biosyst 11 275-286 (2015)


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