Synthesis of N4-(substituted phenyl)-N4-alkyl/ desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells
ANTIPROLIFERATIVE ACTIVITY;
ARTICLE;
CANCER INHIBITION;
CANCER RESISTANCE;
CHLORINATION;
CONTROLLED STUDY;
CYCLIZATION;
DRUG POTENCY;
DRUG SENSITIVITY;
DRUG STRUCTURE;
DRUG SYNTHESIS;
HUMAN;
HUMAN CELL;
MICROTUBULE;
MICROTUBULE ASSEMBLY;
MOLECULAR MODEL;
MULTIDRUG RESISTANCE;
OXIDATION;
TUMOR CELL;
ANILINE COMPOUNDS;
BINDING SITES;
CELL LINE, TUMOR;
CELL PROLIFERATION;
COLCHICINE;
CYCLIZATION;
CYCLOHEXANONES;
DIAMINES;
DRUG RESISTANCE, NEOPLASM;
DRUG SCREENING ASSAYS, ANTITUMOR;
HUMANS;
INDOLES;
MICROTUBULES;
MOLECULAR DOCKING SIMULATION;
OXIDATION-REDUCTION;
PROTEIN BINDING;
PROTEIN STRUCTURE, TERTIARY;
PYRIMIDINES;
TUBULIN MODULATORS;
Aug 28-Sep 1, 2011; Denver, CO, United States, MEDI-53
Gangjee, A.; Zaware, N.; Devambatla, R. K. V.; Mooberry, S. L.; Hamel, E. From Abstracts of Papers, 242nd ACS National Meeting & Exposition, Aug 28-Sep 1, 2011; Denver, CO, United States, MEDI-53.
Combretastatin A4 phosphate in treating patients with advanced solid tumors, http://clinicaltrials.gov/ct2/show/ NCT00003768?term=CA4P&rank=11; Combretastatin A4 phosphate in treating patients with advanced anaplastic thyroid cancer, http://clinicaltrials.gov/ct2/show/ NCT00060242?term= CA4P&rank=9; A safety and efficacy study of carboplatin, paclitaxel, bevacizumab and CA4P in non-small cell lung cancer (FALCON), http://clinicaltrials.gov/ct2/show/ NCT00653939?term=combretastatin&rank=8
Selected clinical trials data for CA4P either alone or in combination: http://www.oxigene.com/pipeline/zybrestat-in-oncology/; Combretastatin A4 phosphate in treating patients with advanced solid tumors, http:// clinicaltrials.gov/ct2/show/NCT00003768?term=CA4P&rank=11; Combretastatin A4 phosphate in treating patients with advanced anaplastic thyroid cancer, http://clinicaltrials.gov/ct2/show/NCT00060242?term=CA4P&rank=9; A safety and efficacy study of carboplatin, paclitaxel, bevacizumab and CA4P in non-small cell lung cancer (FALCON), http://clinicaltrials.gov/ct2/show/NCT00653939?term= combretastatin&rank=8.
Clinical trials: A phase I clinical trial of OXi4503 for relapsed and refractory AML and MDS, http://clinicaltrials.gov/ct2/show/NCT01085656?term= CA1P&rank=1.
P. Skehan, R. Storeng, D. Scudiero, A. Monks, J. McMahon, D. Vistica, J.T. Warren, H. Bokesch, S. Kenney, and M.R. Boyd J. Natl. Cancer Inst. 82 1990 1107
P. Verdier-Pinard, J.-Y. Lai, H.-D. Yoo, J. Yu, B. Marquez, D.G. Nagle, M. Nambu, J.D. White, J.R. Falck, W.H. Gerwick, B.W. Day, and E. Hamel Mol. Pharmacol. 53 1998 62