thiophenes has been researched along with urea in 125 studies
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 12 (9.60) | 18.7374 |
| 1990's | 4 (3.20) | 18.2507 |
| 2000's | 8 (6.40) | 29.6817 |
| 2010's | 85 (68.00) | 24.3611 |
| 2020's | 16 (12.80) | 2.80 |
| Authors | Studies |
|---|---|
| Bulpitt, CJ; Havard, CW; Pearson, RM | 1 |
| Matevosian, AA | 1 |
| Bensted, JP; Calvert, AH; Clinton, S; Hughes, LR; Jodrell, DI; Morgan, SE; Newell, DR | 1 |
| Asaka, M; Iida, H; Izumino, K; Mizumura, Y; Sasayama, S | 1 |
| Cepelák, V; Köcher, P; Opatrný, K; Racek, J | 1 |
| Bouges-Bocquet, B; Delosme, R; Renger, G | 1 |
| Anthony, M; Lance, JW | 1 |
| Fujisawa, T; Muramatsu, M | 1 |
| Anthony, M; Lance, JW; Somerville, B | 1 |
| Henkin, RI | 2 |
| Chapman, NB; Clarke, K; Humphries, AJ; Saraf, SU | 1 |
| Henkin, RI; Hoye, RC | 1 |
| Baxter, GS; Byrne, C; Ellis, ES; Murphy, OE; Tilford, NS | 1 |
| Baxter, GS; Blackburn, TP; Bright, F; Kennett, GA; Trail, B | 1 |
| Lavielle, G; Millan, MJ; Peglion, JL; Perrin-Monneyron, S | 1 |
| Castiglioni, S; Chrambach, A; Eberini, I; Gianazza, E; Rondanini, A; Sirtori, CR; Vecchio, G | 1 |
| Bhargava, A; Bombara, M; Caringal, Y; Dally, R; Dumas, J; Gunn, D; Housley, TJ; Johnson, JS; Kingery-Wood, J; Lee, W; Osterhout, M; Paulsen, H; Ranges, GE; Redman, AM; Renick, J; Scott, WJ; Shrikhande, A; Smith, RA; Swartz, S; Wild, H; Wilhelm, SM; Young, D | 1 |
| Horiuchi, K; Kanai, K; Matsui, Y; Yamamoto, K | 1 |
| Distad, M; Farrugia, G; Gibbons, SJ; Ou, Y; Roeder, JL; Strege, PR; Szurszewski, JH; Wouters, MM | 1 |
| Almeida, L; Ashwell, S; Brassil, PJ; Daly, K; Deng, C; Gero, T; Glynn, RE; Horn, CL; Ioannidis, S; Janetka, JW; Lyne, P; Newcombe, NJ; Oza, VB; Pass, M; Springer, SK; Su, M; Toader, D; Vasbinder, MM; Yu, D; Yu, Y; Zabludoff, SD | 1 |
| Ashwell, S; Caleb, BL; Deng, C; Green, S; Grondine, MR; Haye, HR; Horn, CL; Janetka, JW; Liu, D; Mouchet, E; Queva, C; Ready, S; Rosenthal, JL; Schwartz, GK; Sheehy, AM; Taylor, KJ; Tse, AN; Walker, GE; White, AM; Zabludoff, SD | 1 |
| Baichoo, NS; Bermingham, A; Beutler, J; Bona, MK; Chertov, O; Ehteshami, M; Götte, M; Kvaratskhelia, M; Le Grice, S; Lee, HF; Miller, JT; O'Keefe, BR; Wendeler, M | 1 |
| Ahn, K; Beidler, D; Cravatt, BF; Dunbar, JB; Fay, L; Gregory, T; Johnson, DS; Kesten, S; Lazerwith, SE; Liimatta, M; Morris, M; Nomanbhoy, TK; Smith, S; Song, Y; Stiff, C | 1 |
| Ashwell, S; Brassil, PJ; Dai, J; Garner, CE; Gönen, M; Goteti, K; Kern, SE; Moustakas, DT; Schwartz, GK; Utley, L; Zabludoff, S | 1 |
| Chen, XM; Chen, YD; Li, HF; Liu, HC; Lu, S; Lu, T; Ran, T; Yuan, HL | 1 |
| Conti, C; McNeely, S; Patel, H; Pommier, Y; Schwartz, G; Sheikh, T; Tse, A; Zabludoff, S | 1 |
| Choudhuri, R; Citrin, D; Cook, JA; Fabre, K; Mitchell, JB; Sowers, AL; Zabludoff, SD | 1 |
| Dai, Y; Grant, S | 1 |
| Arumugarajah, S; Canman, CE; Davis, MA; Hassan, MC; Hylander-Gans, L; Lawrence, TS; Maybaum, J; Morgan, MA; Morosini, D; Normolle, DP; Parsels, JD; Parsels, LA; Simeone, DM; Zabludoff, SD; Zhao, L | 1 |
| Dent, P; Eulitt, P; Mitchell, C; Park, M; Yacoub, A; Yang, C | 1 |
| Caivano, AR; Decker, ER; Dixon, RA; Lejeune, WS; McIntyre, BW; Miyamoto, YJ; Munsch, CL; Sherwood, SJ; Tilton, RG; Vanderslice, P; Woodside, DG | 1 |
| Lawrence, TS; Maybaum, J; Morgan, MA; Normolle, D; Parsels, LA; Zhao, L | 1 |
| Cheung, IY; Cheung, NK; Gao, X; Tran, H; Wei, XX; Xu, H | 1 |
| Alton, G; Connolly, B; Juan, M; Kablaoui, NM; Kuhn, C; Liu, H; Sharma, R; Stanton, R; Ye, P | 1 |
| Choi, SH; Jin, J; Lee, JI; Nam, DH; Seol, HJ; Yang, H; Yoo, HY; Yoon, SJ | 1 |
| Battistella, A; Escargueil, AE; Henriques, JA; Larsen, AK; Matuo, R; Rocca, CJ; Soares, DG | 1 |
| Arumugarajah, S; Brown, JL; Gross, M; Hassan, MC; Hylander-Gans, L; Lawrence, TS; Maybaum, J; Morgan, MA; Morosini, D; Parsels, JD; Parsels, LA; Qian, Y; Simeone, DM; Tanska, DM; Zabludoff, SD; Zhao, L | 1 |
| Blasius, M; Forment, JV; Guerini, I; Jackson, SP | 1 |
| Almenara, JA; Bodie, WW; Chen, S; Dai, Y; Dent, P; Felthousen, J; Grant, S; Kramer, LB; Pei, XY; Takabatake, Y; Youssefian, LE | 1 |
| Forshell, LP; Höglund, A; Li, Y; Nilsson, JA; Strömvall, K | 1 |
| Choy, ML; Lee, JH; Marks, PA; Ngo, L; Venta-Perez, G | 1 |
| Brown, JL; Lawrence, TS; Liu, E; Maybaum, J; Morgan, MA; Parsels, JD; Parsels, LA; Vance, S; Zhao, L | 1 |
| Aris, SM; Pommier, Y | 1 |
| Demur, C; Didier, C; Ducommun, B; Grimal, F; Jullien, D; Manenti, S | 1 |
| Brown, EJ; Schoppy, DW | 1 |
| Aft, RL; Cai, S; Ellis, MJ; Goiffon, RJ; Guo, Z; Hoog, J; Li, S; Lin, L; Ma, CX; Piwnica-Worms, H; Prat, A; Ryan, CE; Schaiff, WT | 1 |
| Almeida, L; Ashwell, S; Brassil, P; Breed, J; Deng, C; Gero, T; Grondine, M; Horn, C; Ioannidis, S; Janetka, J; Liu, D; Lyne, P; Newcombe, N; Oza, V; Pass, M; Read, J; Ready, S; Rowsell, S; Su, M; Toader, D; Vasbinder, M; Xue, Y; Yu, D; Yu, Y; Zabludoff, S | 1 |
| Aarts, M; Ashworth, A; Garcia-Murillas, I; Gevensleben, H; Hurd, MS; Sharpe, R; Shumway, SD; Toniatti, C; Turner, NC | 1 |
| Asai, T; Comenzo, RL; Friedman, H; Jhanwar, SC; Landau, HJ; McNeely, SC; Nair, JS; Nimer, SD; Schwartz, GK | 1 |
| Fan, Y; Feng, X; Gao, S; Ma, Z; Yao, G; Zhou, B | 1 |
| Bepler, G; Chen, Z; Li, X; Malysa, A; Oliveira, P; Zhang, Y; Zhou, J | 1 |
| Alves, MV; Fitzgerald, AL; Frederick, MJ; Gadhikar, MA; Myers, JN; Neskey, DM; Osman, AA; Pickering, CR; Sciuto, MR; Zhao, M | 1 |
| Agbo, F; Arita, S; Esaki, T; Fujimoto, C; Hamatake, M; Hirai, F; Kometani, T; Makiyama, A; Nosaki, K; Seto, T; Shi, X; Takeoka, H | 1 |
| Harada, T; Itamochi, H; Kato, M; Kigawa, J; Kudoh, A; Naniwa, J; Nishimura, M; Oishi, T; Oumi, N; Sato, S; Shimada, M | 1 |
| Beer, DG; Bergeron, EJ; Chen, G; Giordano, TJ; Grabauskiene, S; Morgan, MA; Reddy, RM; Thomas, DG | 1 |
| Agbo, F; Azad, N; Barker, P; Carducci, M; Carter, J; Cosgrove, D; Knight, R; Lorusso, P; Malburg, L; Oakes, P; Quinn, MF; Sausville, E; Senderowicz, A; Zabludoff, S | 1 |
| Aparicio, AM; Broom, B; Chang, W; Corn, PG; Dobashi, M; Efstathiou, E; Karanika, S; Karantanos, T; Lee, HS; Lee, JS; Li Ning Tapia, EM; Li, L; Maity, SN; Navone, N; Park, S; Ren, C; Shah, PK; Takahiro, H; Thompson, TC; Troncoso, P; Wang, J; Xiao, L; Yang, G; Yin, J; Zhang, W | 1 |
| Biediger, RJ; Bonig, H; Esguerra, ZA; Gang, EJ; Hsieh, YT; Jang, J; Khazal, S; Kim, HN; Kim, YM; Kwok, E; Osborne, A; Pham, J; Shishido, SN; Vanderslice, P | 1 |
| Hematulin, A; Sagan, D; Sawanyawisuth, K; Seubwai, W; Wongkham, S | 1 |
| Bryant, C; Massey, AJ; Rawlinson, R | 1 |
| de Vries, EG; Fehrmann, RS; Franke, L; Krajewska, M; Labib, S; Schoonen, PM; van Vugt, MA | 1 |
| Ma, HT; Mak, JP; Man, WY; Poon, RY | 1 |
| Kwiatkowski, DJ; Liu, Y | 1 |
| Lee, BH; Lim, CJ; Oh, KS; Oh, SA; Yi, KY | 1 |
| Agostinelli, C; Brighenti, E; Casadei, B; Derenzini, E; Ferrari, A; Fuligni, F; Ghelli Luserna Di Rorà, A; Iacobucci, I; Imbrogno, E; Martinelli, G; Pileri, S; Righi, S; Zinzani, PL | 1 |
| Da-Rè, C; Halazonetis, TD | 1 |
| Baranski, Z; Booij, TH; Bovée, JV; Cleton-Jansen, AM; Danen, EH; Hogendoorn, PC; Price, LS; van de Water, B | 1 |
| Börger, C; Empting, M; Groh, M; Hartmann, RW; Kamal, A; Sahner, JH; Weidel, E | 1 |
| Ahluwalia, D; Bhupathi, D; Hart, CP; Liu, Q; Matteucci, MD; Meng, F; Sun, JD; Wang, Y | 1 |
| Chow, JP; Ma, HT; Mak, JP; Man, WY; Poon, RY | 1 |
| Emilsen, E; Engesæter, B; Fjær, R; Flørenes, VA; Giller Fleten, K; Magnussen, GI; Nähse-Kumpf, V; Slipicevic, A | 1 |
| Bojorquez-Gomez, A; Gross, A; Ideker, T; Jaehnig, EJ; Klepper, K; Li, J; Licon, K; Pekin, D; Qiu, CP; Shen, JP; Sivaganesh, V; Sobol, RW; Srivas, R; Sun, SM; van Attikum, H; Xu, JL; Yeerna, H | 1 |
| Bertoni, F; Carrassa, L; Chilà, R; Damia, G; Kwee, I; Lupi, M; Restelli, V; Rinaldi, A | 1 |
| Cuneo, KC; Lawrence, TS; Maybaum, J; Morgan, MA; Parsels, JD; Parsels, LA; Tanska, DM; Zabludoff, SD | 1 |
| Babich, JW; Mairs, RJ; Nixon, C; Rae, C; Tesson, M | 1 |
| Machado, VA; Peixoto, D; Queiroz, MJ; Soares, R | 1 |
| Deng, O; Du, Z; Gao, J; Gorityala, S; Lai, J; Ma, Z; Susana, G; Xiong, X; Xu, Y; Yan, C; Yang, S; Zhang, J; Zhang, Y | 1 |
| Green, JE; He, S; Min, DJ | 1 |
| Alimova, I; Balakrishnan, I; Birks, DK; Davidson, N; Donson, AM; Foreman, NK; Griesinger, AM; Handler, MH; Harris, PS; Mulcahy Levy, JM; Prince, EW; Remke, M; Shah, M; Taylor, MD; Venkataraman, S; Vibhakar, R | 1 |
| Aryal, DK; Bernat, V; Corder, G; Dengler, D; Giguère, PM; Gmeiner, P; Huang, XP; Hübner, H; Kling, RC; Kobilka, BK; Levit, A; Lin, H; Löber, S; Manglik, A; McCorvy, JD; Roth, BL; Sassano, MF; Scherrer, G; Shoichet, BK | 1 |
| Cho, JH; Choi, HG; Kim, CY; Kim, D; Kim, HK; Kim, ND; Ko, E; Lee, C; Lee, SH; Nan, HY; Park, JS; Son, JB; Yoon, S | 1 |
| Bago-Horvath, Z; Fece de la Cruz, F; Haura, EB; Katz, AM; Kerzendorfer, C; Konopka, T; Loizou, JI; Mair, B; Mazouzi, A; Muellner, MK; Nagy-Bojarszky, K; Nijman, SM; Paz, K; Smida, M; Suchankova, T; Uras, IZ | 1 |
| Arribas, AJ; Bertoni, F; Carrassa, L; Damia, G; Restelli, V; Vagni, M | 1 |
| Hasvold, G; Hauge, S; Joel, M; Juzenas, P; Naucke, C; Rødland, GE; Stokke, T; Syljuåsen, RG | 1 |
| Cinatl, J; Hoffmann, MJ; Isono, M; Michaelis, M; Niegisch, G; Pinkerneil, M; Sato, A; Schulz, WA | 1 |
| Ebeid, K; Ho, GN; Salem, AK | 1 |
| Frederick, M; Johnson, FM; Kalu, NN; Li, L; Mazumdar, T; Myers, JN; Peng, S; Pickering, CR; Sambandam, V; Shen, L; Singh, R; Tong, P; Wang, J; Zhang, M | 1 |
| Bravo Sagua, R; Busso, D; Cárdenas, C; Cataldo, LR; Cortés, VA; Galgani, JE; Jaña, F; Llanos, P; Mizgier, ML; Olmos, P; Santos, JL | 1 |
| Aparicio, AM; Broom, B; Corn, PG; Gallick, GE; Karanika, S; Karantanos, T; Li, L; Li, S; Maity, SN; Manyam, GC; Navone, N; Park, S; Song, JH; Thompson, TC; Troncoso, P; Wang, J; Yang, G; Zhang, W; Zuo, X | 1 |
| Dong, X; Lv, J; Ni, X; Qian, Y; Xu, X | 1 |
| Aguilar-Bonavides, C; Behrens, C; Çeliktas, M; Delgado, O; Dennison, JB; Dhillon, D; Do, KA; Fahrmann, JF; Gazdar, AF; Hanash, SM; Ostrin, EJ; Taguchi, A; Tanaka, I; Tripathi, SC; Villalobos, P; Wang, H | 1 |
| Camurlu, P; Cevik, E; Dervisevic, E; Dervisevic, M; Senel, M; Yildiz, HB | 1 |
| Benes, C; Gao, P; Gray, NS; Li, F; Li, Y; Liu, F; Liu, Q; Liu, Y; Merlino, AA; Quinn, MM; Wang, X; Wong, KK | 1 |
| Chen, X; Chowdhury, S; Groppi, VE; Herr, RJ; Jiang, Q; Johnson, G; Owens, KN; Raible, DW; Rubel, EW; Simon, JA | 1 |
| Jin, J; Lei, H; Li, X; Liu, M; Luo, H; Wu, Y; Xu, H; Yang, L | 1 |
| Che, Y; He, J; Li, N; Li, Y; Lu, ZL; Puno, PT; Sun, HD; Sun, N; Wan, J; Wang, JN; Yuan, ZY; Zhang, ZR | 1 |
| Bailey, C; Conibear, A; Dewey, W; Disney, A; Henderson, G; Hill, R; Husbands, S; Kelly, E; Sutcliffe, K | 1 |
| Braisted, JC; Chan, DW; Chen, CW; Cheung, ANY; Dai, Z; Kai, Y; Li, J; Li, Y; Li, Z; Liu, SS; Meng, Y; Ngan, HYS; Peng, W; Sun, J; Sun, W; Tzatsos, A; Yung, MMH; Zheng, W; Zhou, W; Zhu, W | 1 |
| Blümel, L; Bormann, S; Fritz, G; Geist, K; Honnen, S; Klöcker, N; Krüger, K; Remke, M; Roos, WP; Schumacher, L; Stork, B; Stuhldreier, F; Wesselborg, S | 1 |
| Livingston, KE; Mahoney, JP; Manglik, A; Sunahara, RK; Traynor, JR | 1 |
| Chen, A; Guo, Y; Jalali, A; Li, BY; Liu, S; Na, S; Nakshatri, H; Wang, L; Wang, Y; Yokota, H | 1 |
| Carroll, KR; Elfers, EE; Hildeman, DA; Jordan, MB; Katz, JD; McNally, JP; Stevens, JJ | 1 |
| Araldi, D; Ferrari, LF; Levine, JD | 1 |
| Che, Y; He, J; Li, N; Li, RD; Li, Y; Lu, ZL; Puno, PT; Sun, HD; Sun, N; Wan, J; Wang, JN; Yuan, ZY; Zhang, ZR | 1 |
| Cen, X; Chen, Z; Cheng, K; Lin, Z; Liu, M; Yang, J | 1 |
| Cai, L; Guo, Y; Li, A; Li, J; Li, Q; Miao, Y; Tian, H; Wang, L; Xie, M; Zhang, X; Zhao, J | 1 |
| Benyhe, S; Bojarski, AJ; Buda, S; Bugno, R; Golembiowska, K; Kudla, L; Makuch, W; Przewlocka, B; Przewlocki, R; Skupio, U; Solecki, W; Wiktorowska, L; Wojtas, A; Zádor, F | 1 |
| Camci, ED; Gibson, RM; Kirkwood, NK; Kitcher, SR; Kros, CJ; Raible, DW; Redila, VA; Richardson, GP; Rubel, EW; Simon, JA; Wu, P | 1 |
| Flem-Karlsen, K; Flørenes, VA; Gullestad, HP; Haugen, MH; Hermann, R; McFadden, E; Mælandsmo, GM; Omar, N; Ryder, T; Øy, GF | 1 |
| Alamein, C; Canals, M; Christie, MJ; Connor, M; Fritzwanker, S; Gillis, A; Gondin, AB; Grimsey, NL; Halls, ML; Kassiou, M; Katte, TA; Kellam, B; Kliewer, A; Krasel, C; Lane, JR; Lim, HD; Manandhar, P; Reekie, T; Sanchez, J; Santiago, M; Schmiedel, F; Schulz, S | 1 |
| Chao, HH; Facciabene, A; François, NB; Karagounis, IV; Koumenis, C; Maity, A; Thomas, C | 1 |
| Huang, T; Li, J; Zhao, Z | 1 |
| Cannavò, D; Caraci, F; Caruso, G; Drago, F; Leggio, GM; Salomone, S; Santagati, M | 1 |
| Czoty, PW; Ding, H; Hsu, FC; Kiguchi, N; Ko, MC; Nguyen, T; Perrey, DA; Zhang, Y | 1 |
| Chen, W; Jin, X; Li, F; Li, H; Li, Q; Liu, B | 1 |
| Chen, Y; Tsai, YH; Tseng, BJ; Tseng, SH | 1 |
| Bojarski, AJ; Bugno, R; Kudla, L; Podlewska, S; Przewlocki, R | 1 |
| Bae, SH; Bong, SM; Jang, H; Lee, BI; Park, TH; Ryu, SE | 1 |
| Jaswal, S; Kumar, S; Monga, V; Rulhania, S | 1 |
| Bong, D; Floyd, C; Liao, S; Pino, MJ; Tan, K; Wu, C | 1 |
| Choi, I; Kim, TK; Lee, EK; Lim, JW; Ryu, HC; Windisch, M; Yoo, HH | 1 |
| Adekoya, P; Gulati, A; Hunter, C; Jones, MR; Kaye, AD; Kaye, AM; Kuppalli, S; Orhurhu, V; Seth, R; Urits, I | 1 |
| Agostinelli, C; Alcalay, M; Baiardi, E; Bertolini, F; Calleri, A; Casadei, B; Corsini, C; Derenzini, E; Falvo, P; Fiori, S; Mazzara, S; Melle, F; Motta, G; Orecchioni, S; Pelicci, PG; Pileri, S; Rossi, A; Tabanelli, V; Tarella, C; Vitolo, U; Zinzani, PL | 1 |
| Hao, GZ; Jiang, CS; Li, Y; Liu, SK; Xie, HX; Zhang, J; Zhang, JH; Zheng, H; Zhu, KK | 1 |
3 review(s) available for thiophenes and urea
| Article | Year |
|---|---|
New antipsychotic drugs for the treatment of agitation and psychosis in Alzheimer's disease: focus on brexpiprazole and pimavanserin.
Topics: Alzheimer Disease; Antipsychotic Agents; Anxiety; Humans; Piperidines; Psychotic Disorders; Quinolones; Thiophenes; Urea | 2020 |
Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors.
Topics: Acetazolamide; Animals; Antineoplastic Agents; Antioxidants; Benzenesulfonamides; Carbonic Anhydrase Inhibitors; Carbonic Anhydrases; Humans; Indoles; Isatin; Molecular Docking Simulation; Organoselenium Compounds; Oxadiazoles; Protein Binding; Protein Isoforms; Pyrimidines; Structure-Activity Relationship; Sulfonamides; Thiazines; Thiophenes; Urea | 2021 |
Recent Advances in the Treatment of Opioid Use Disorder.
Topics: Analgesics, Opioid; Buprenorphine; Delayed-Action Preparations; Drug Implants; Humans; Injections, Intramuscular; Methadone; Molecular Targeted Therapy; Naltrexone; Narcotic Antagonists; Opiate Substitution Treatment; Opioid-Related Disorders; Receptors, G-Protein-Coupled; Receptors, Opioid, mu; Secologanin Tryptamine Alkaloids; Thiophenes; Urea; Vaccines | 2021 |
6 trial(s) available for thiophenes and urea
| Article | Year |
|---|---|
Biochemical and haematological changes induced by tienilic acid combined with propranolol in essential hypertension.
Topics: Adult; Aged; Blood Pressure; Blood Sedimentation; Clinical Trials as Topic; Creatinine; Diuretics; Double-Blind Method; Drug Synergism; Drug Therapy, Combination; Female; Glycolates; Hemoglobins; Humans; Hypertension; Leukocyte Count; Male; Middle Aged; Phenoxyacetates; Potassium; Propranolol; Thiophenes; Urea; Uric Acid | 1979 |
[Comparative evaluation of the new antiserotonin preparations, sandomigran and lizenil, in treating patients suffering from migraine].
Topics: Adult; Cerebrovascular Circulation; Chronic Disease; Clinical Trials as Topic; Czechoslovakia; Drug Evaluation; Ergolines; Female; Humans; Male; Middle Aged; Migraine Disorders; Pizotyline; Serotonin Antagonists; Sweden; Thiophenes; Urea | 1976 |
A comparative trial of serotonin antagonists in the management of migraine.
Topics: Clinical Trials as Topic; Cyproheptadine; Ergolines; Humans; Methysergide; Migraine Disorders; Phenothiazines; Placebos; Serotonin Antagonists; Thiophenes; Urea | 1970 |
Phase I, dose-escalation study of AZD7762 alone and in combination with gemcitabine in Japanese patients with advanced solid tumours.
Topics: Aged; Antineoplastic Combined Chemotherapy Protocols; Checkpoint Kinase 1; Checkpoint Kinase 2; Deoxycytidine; Dose-Response Relationship, Drug; Female; Gemcitabine; Humans; Japan; Male; Maximum Tolerated Dose; Middle Aged; Neoplasms; Protein Kinases; Protein Serine-Threonine Kinases; Thiophenes; Urea | 2013 |
Phase I dose-escalation study of AZD7762, a checkpoint kinase inhibitor, in combination with gemcitabine in US patients with advanced solid tumors.
Topics: Adult; Aged; Antimetabolites, Antineoplastic; Antineoplastic Combined Chemotherapy Protocols; Checkpoint Kinase 1; Deoxycytidine; Dose-Response Relationship, Drug; Female; Gemcitabine; Humans; Male; Middle Aged; Neoplasms; Protein Kinases; Thiophenes; Urea | 2014 |
Dual targeting of the DNA damage response pathway and BCL-2 in diffuse large B-cell lymphoma.
Topics: Adolescent; Adult; Aged; Aged, 80 and over; Antineoplastic Agents; Biomarkers, Tumor; Bridged Bicyclo Compounds, Heterocyclic; DNA Repair Enzymes; Drug Therapy, Combination; Female; Follow-Up Studies; Gene Expression Regulation, Leukemic; Humans; Lymphoma, Large B-Cell, Diffuse; Male; Middle Aged; Prognosis; Prospective Studies; Proto-Oncogene Proteins c-bcl-2; Retrospective Studies; Sulfonamides; Survival Rate; Thiophenes; Urea; Young Adult | 2022 |
116 other study(ies) available for thiophenes and urea
| Article | Year |
|---|---|
The renal effects of N10-propargyl-5,8-dideazafolic acid (CB3717) and a non-nephrotoxic analogue ICI D1694, in mice.
Topics: Animals; Carbon Radioisotopes; Cisplatin; Creatinine; Female; Folic Acid; Glomerular Filtration Rate; Inulin; Kidney; Kidney Diseases; Male; Mice; Mice, Inbred BALB C; Mice, Inbred DBA; Quinazolines; Thiophenes; Thymidylate Synthase; Urea | 1991 |
Effect of the antiplatelet agents ticlopidine and dipyridamole on experimental immune complex glomerulonephritis in rats.
Topics: Animals; Antibodies; Antigen-Antibody Complex; Cattle; Creatinine; Dipyridamole; Fluorescent Antibody Technique; Glomerulonephritis; Immune Complex Diseases; Injections, Subcutaneous; Kidney Function Tests; Male; Platelet Aggregation; Proteinuria; Rats; Rats, Inbred SHR; Rats, Inbred Strains; Serum Albumin, Bovine; Thiophenes; Ticlopidine; Time Factors; Urea | 1986 |
[Influencing the effectiveness of repeatedly used dialyzers by the administration of ticlopidine (Ticlid)].
Topics: Adult; Blood Platelets; Creatinine; Female; Heparin; Humans; Male; Renal Dialysis; Thiophenes; Ticlopidine; Urea | 1986 |
Studies on the ADRY agent-induced mechanism of the discharge of the holes trapped in the photosynthetic watersplitting enzyme system Y.
Topics: Actinium; Aniline Compounds; Chloroplasts; Electron Transport; Kinetics; Luminescent Measurements; Mathematics; Models, Biological; Nitro Compounds; Oxygen; Photosynthesis; Plant Cells; Plants; Polarography; Spectrometry, Fluorescence; Thiophenes; Time Factors; Urea; Water | 1973 |
Studies on the sedimentation properties of nuclear, nuclelar and extranucleolar nuclear RNA.
Topics: Amylases; Animals; Carbon Isotopes; Cell Nucleolus; Cell Nucleus; Centrifugation, Density Gradient; Deoxyribonucleases; Edetic Acid; Hydrogen-Ion Concentration; Liver; Molecular Weight; Orotic Acid; Peptide Hydrolases; Rats; RNA; Sulfones; Thiophenes; Tritium; Urea | 1968 |
Thermographic, hormonal, and clinical studies in migraine.
Topics: Body Temperature; Cycloheptanes; Cyproheptadine; Ergolines; Female; Humans; Menstruation; Methysergide; Migraine Disorders; Phenothiazines; Piperidines; Progesterone; Reserpine; Serotonin Antagonists; Skin Temperature; Thermography; Thiophenes; Urea | 1970 |
Impairment of olfaction and of the tastes of sour and bitter in pseudohypoparathyroidism.
Topics: Adolescent; Adult; Calcium; Female; Humans; Hydrochloric Acid; Male; Nitrobenzenes; Parathyroid Hormone; Phosphates; Pseudohypoparathyroidism; Pyridines; Smell; Sodium Chloride; Sucrose; Taste; Thiophenes; Turner Syndrome; Urea | 1968 |
Pharmacologically active benzo[b]thiophen derivatives. VII. Analogues of tryptamine and heteroauxin.
Topics: Amides; Antineoplastic Agents; Ethylamines; Guanidines; Plant Growth Regulators; Sulfur; Thiophenes; Tryptamines; Urea | 1969 |
Hyposmia secondary to excision of the olfactory epithelium. The definition of primary and accessory areas of olfaction.
Topics: Female; Humans; Hydrochloric Acid; Hydroxides; Male; Middle Aged; Nasal Mucosa; Nitrobenzenes; Olfaction Disorders; Paranasal Sinus Neoplasms; Pyridines; Quaternary Ammonium Compounds; Sodium Chloride; Sucrose; Taste; Thiophenes; Urea | 1966 |
Abnormalities of taste and olfaction in patients with chromatin negative gonadal dysgenesis.
Topics: Adolescent; Adult; Child; Female; Humans; Hydrochloric Acid; Male; Nitrobenzenes; Pharmacogenetics; Psychopharmacology; Pyridines; Sex Chromatin; Smell; Sodium Chloride; Sucrose; Taste; Thiophenes; Turner Syndrome; Urea | 1967 |
Mediation by 5-hydroxytryptamine2B receptors of endothelium-dependent relaxation in rat jugular vein.
Topics: Animals; Carbachol; Endothelium, Vascular; In Vitro Techniques; Indoles; Jugular Veins; Male; Mianserin; Muscle Relaxation; Muscle, Smooth, Vascular; Rats; Rats, Sprague-Dawley; Receptors, Serotonin; Serotonin; Serotonin Antagonists; Serotonin Receptor Agonists; Thiophenes; Urea; Yohimbine | 1995 |
Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety.
Topics: Animals; Anti-Anxiety Agents; Anxiety; Behavior, Animal; Chlordiazepoxide; Disease Models, Animal; Indoles; Male; Rats; Rats, Sprague-Dawley; Serotonin Receptor Agonists; Thiophenes; Urea | 1996 |
5-HT2C receptors mediate penile erections in rats: actions of novel and selective agonists and antagonists.
Topics: Animals; Dose-Response Relationship, Drug; Ethylamines; Indoles; Male; Penile Erection; Piperazines; Pyridines; Rats; Rats, Wistar; Receptor, Serotonin, 5-HT2C; Receptors, Serotonin; Serotonin Antagonists; Serotonin Receptor Agonists; Thiophenes; Urea | 1997 |
Interactions between carbonic anhydrase and its inhibitors revealed by gel electrophoresis and circular dichroism.
Topics: Acetazolamide; Animals; Carbonic Anhydrase Inhibitors; Carbonic Anhydrases; Cattle; Circular Dichroism; Electrophoresis, Polyacrylamide Gel; Isoelectric Focusing; Methazolamide; Sodium Dodecyl Sulfate; Sulfonamides; Thiophenes; Titrimetry; Urea | 2000 |
p38 kinase inhibitors for the treatment of arthritis and osteoporosis: thienyl, furyl, and pyrrolyl ureas.
Topics: Arthritis; Enzyme Inhibitors; Furans; Humans; Inhibitory Concentration 50; Interleukin-6; Mitogen-Activated Protein Kinases; Molecular Structure; Osteoporosis; p38 Mitogen-Activated Protein Kinases; Pyrroles; Thiophenes; Tumor Cells, Cultured; Urea | 2001 |
Pharmacological properties of R-755, a novel acyl-CoA:cholesterol acyltransferase inhibitor, in cholesterol-fed rats, hamsters and rabbits.
Topics: Anilides; Animals; Aorta, Thoracic; Arteriosclerosis; Cholesterol; Cholesterol, Dietary; Cricetinae; Dose-Response Relationship, Drug; Enzyme Inhibitors; Humans; Hypolipidemic Agents; Liver; Male; Mesocricetus; Microsomes; Rabbits; Rats; Rats, Sprague-Dawley; Sterol O-Acyltransferase; Thiophenes; Triglycerides; Tumor Cells, Cultured; Urea | 2001 |
Exogenous serotonin regulates proliferation of interstitial cells of Cajal in mouse jejunum through 5-HT2B receptors.
Topics: Animals; Cell Proliferation; Cell Survival; Coculture Techniques; Indoles; Jejunum; Mice; Mice, Inbred BALB C; Mice, Inbred Strains; Myocytes, Smooth Muscle; Receptor, Serotonin, 5-HT2B; Ritanserin; RNA, Messenger; Serotonin; Serotonin 5-HT2 Receptor Agonists; Serotonin Agents; Serotonin Antagonists; Thiophenes; Urea | 2007 |
Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors.
Topics: Amides; Apoptosis; Carbon; Cell Cycle; Checkpoint Kinase 1; Chemistry, Pharmaceutical; DNA Damage; Drug Design; Humans; Inhibitory Concentration 50; Models, Chemical; Phenyl Ethers; Protein Kinase Inhibitors; Protein Kinases; Thiophenes; Urea | 2008 |
AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies.
Topics: Animals; Biological Assay; Cell Cycle Proteins; Cell Death; Checkpoint Kinase 1; Deoxycytidine; DNA Damage; DNA, Neoplasm; Drug Synergism; G2 Phase; Gemcitabine; HCT116 Cells; HT29 Cells; Humans; Male; Mice; Mutation; Protein Kinase Inhibitors; Protein Kinases; Rats; Thiophenes; Topotecan; Tumor Suppressor Protein p53; Urea; Xenograft Model Antitumor Assays | 2008 |
Vinylogous ureas as a novel class of inhibitors of reverse transcriptase-associated ribonuclease H activity.
Topics: Binding Sites; Combinatorial Chemistry Techniques; Furans; HIV Reverse Transcriptase; Humans; Reverse Transcriptase Inhibitors; Ribonuclease H, Human Immunodeficiency Virus; Thiophenes; Urea | 2008 |
Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH).
Topics: Amidohydrolases; Animals; Computer Simulation; Enzyme Inhibitors; Humans; Models, Chemical; Piperazines; Piperidines; Rats; Structure-Activity Relationship; Thiophenes; Urea | 2009 |
Preclinical pharmacokinetic/pharmacodynamic models to predict synergistic effects of co-administered anti-cancer agents.
Topics: Algorithms; Animals; Antineoplastic Agents, Phytogenic; Antineoplastic Combined Chemotherapy Protocols; Camptothecin; Cell Proliferation; Drug Evaluation, Preclinical; Drug Synergism; Flavonoids; Genes, cdc; Growth Inhibitors; Humans; Irinotecan; Mice; Mice, Nude; Models, Statistical; Neoplasm Transplantation; Piperidines; Predictive Value of Tests; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2010 |
Structure-based and shape-complemented pharmacophore modeling for the discovery of novel checkpoint kinase 1 inhibitors.
Topics: Benzodiazepinones; Binding Sites; Biocatalysis; Checkpoint Kinase 1; Drug Design; Ligands; Models, Molecular; Molecular Structure; Pharmaceutical Preparations; Protein Binding; Protein Kinase Inhibitors; Protein Kinases; Protein Structure, Tertiary; Pyrazoles; Staurosporine; Structure-Activity Relationship; Thiophenes; Urea | 2010 |
Chk1 inhibition after replicative stress activates a double strand break response mediated by ATM and DNA-dependent protein kinase.
Topics: Ataxia Telangiectasia Mutated Proteins; Cell Cycle Proteins; Cell Line, Tumor; Checkpoint Kinase 1; Comet Assay; Deoxycytidine; DNA Breaks, Double-Stranded; DNA Repair; DNA-Activated Protein Kinase; DNA-Binding Proteins; G1 Phase; Gemcitabine; Histones; Humans; Mitosis; Protein Kinase Inhibitors; Protein Kinases; Protein Serine-Threonine Kinases; RNA Interference; RNA, Small Interfering; S Phase; Thiophenes; Tumor Suppressor Proteins; Urea | 2010 |
In vitro and in vivo radiation sensitization of human tumor cells by a novel checkpoint kinase inhibitor, AZD7762.
Topics: Animals; Cells, Cultured; Checkpoint Kinase 1; DNA Damage; Dose-Response Relationship, Drug; Female; G2 Phase; HT29 Cells; Humans; Mice; Mice, Nude; Mitotic Index; Neoplasms; Protein Kinase Inhibitors; Protein Kinases; Radiation Tolerance; Radiation-Sensitizing Agents; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2010 |
Targeting Chk1 in the replicative stress response.
Topics: Checkpoint Kinase 1; DNA Breaks, Double-Stranded; DNA Repair; DNA Replication; Drug Synergism; Humans; Protein Kinase Inhibitors; Protein Kinases; Signal Transduction; Stress, Physiological; Thiophenes; Urea | 2010 |
Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair.
Topics: Adenocarcinoma; Animals; Blotting, Western; Cell Line, Tumor; Checkpoint Kinase 1; Checkpoint Kinase 2; Deoxycytidine; DNA Damage; DNA Repair; Drug Therapy, Combination; Flow Cytometry; Fluorescent Antibody Technique; G2 Phase; Gamma Rays; Gemcitabine; Humans; Immunoblotting; Immunoenzyme Techniques; Mice; Mice, Inbred NOD; Mice, SCID; Pancreatic Neoplasms; Protein Kinase Inhibitors; Protein Kinases; Protein Serine-Threonine Kinases; Rad51 Recombinase; Radiation-Sensitizing Agents; Recombination, Genetic; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2010 |
Poly(ADP-ribose) polymerase 1 modulates the lethality of CHK1 inhibitors in carcinoma cells.
Topics: Cell Death; Cell Line, Tumor; Checkpoint Kinase 1; Drug Synergism; Enzyme Activation; Histones; Humans; Mitogen-Activated Protein Kinase 1; Mitogen-Activated Protein Kinase 3; Phosphorylation; Poly (ADP-Ribose) Polymerase-1; Poly(ADP-ribose) Polymerase Inhibitors; Poly(ADP-ribose) Polymerases; Protein Kinase Inhibitors; Protein Kinases; Signal Transduction; Staurosporine; Thiophenes; Urea | 2010 |
Potent in vivo suppression of inflammation by selectively targeting the high affinity conformation of integrin α4β1.
Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Humans; Hypersensitivity; Inflammation; Integrin alpha4beta1; Jurkat Cells; Lymphocyte Activation; Mice; Protein Conformation; Pulmonary Eosinophilia; T-Lymphocytes; Thiophenes; Urea | 2010 |
Bayesian hierarchical changepoint methods in modeling the tumor growth profiles in xenograft experiments.
Topics: Animals; Bayes Theorem; Cell Proliferation; Confidence Intervals; Deoxycytidine; Gemcitabine; Mice; Models, Biological; Models, Statistical; Neoplasms; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2011 |
Checkpoint kinase inhibitor synergizes with DNA-damaging agents in G1 checkpoint-defective neuroblastoma.
Topics: Animals; Antimetabolites, Antineoplastic; Cell Line, Tumor; Checkpoint Kinase 1; Checkpoint Kinase 2; Deoxycytidine; DNA Damage; Drug Resistance, Neoplasm; Drug Synergism; Female; Gemcitabine; Humans; Mice; Mice, Nude; Neuroblastoma; Protein Kinase Inhibitors; Protein Kinases; Protein Serine-Threonine Kinases; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2011 |
Potent and selective thiophene urea-templated inhibitors of S6K.
Topics: Humans; Microsomes, Liver; Protein Kinase Inhibitors; Ribosomal Protein S6 Kinases, 70-kDa; Structure-Activity Relationship; Thiophenes; Urea | 2011 |
Inhibition of checkpoint kinase 1 sensitizes lung cancer brain metastases to radiotherapy.
Topics: Animals; Brain Neoplasms; Cell Line, Tumor; Checkpoint Kinase 1; Gene Deletion; Humans; Lung Neoplasms; Male; Mice; Mice, Nude; Neoplasm Metastasis; Protein Kinase Inhibitors; Protein Kinases; Radiation Tolerance; RNA, Small Interfering; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2011 |
Ataxia telangiectasia mutated- and Rad3-related kinase drives both the early and the late DNA-damage response to the monofunctional antitumour alkylator S23906.
Topics: Acid Anhydride Hydrolases; Acronine; Antineoplastic Agents, Alkylating; Ataxia Telangiectasia Mutated Proteins; Cell Cycle Proteins; Checkpoint Kinase 1; Checkpoint Kinase 2; DNA Damage; DNA Repair Enzymes; DNA-Binding Proteins; HeLa Cells; Histones; Humans; Microscopy, Fluorescence; MRE11 Homologue Protein; Mutation; Nuclear Proteins; Protein Kinases; Protein Serine-Threonine Kinases; Replication Protein A; Thiophenes; Urea | 2011 |
Assessment of chk1 phosphorylation as a pharmacodynamic biomarker of chk1 inhibition.
Topics: Animals; Biomarkers; Cell Line, Tumor; Cell Survival; Checkpoint Kinase 1; Deoxycytidine; DNA Damage; Gemcitabine; Histones; Humans; Mice; Pancreatic Neoplasms; Phosphorylation; Protein Kinase Inhibitors; Protein Kinases; Thiophenes; Transplantation, Heterologous; Urea; Xenograft Model Antitumor Assays | 2011 |
Structure-specific DNA endonuclease Mus81/Eme1 generates DNA damage caused by Chk1 inactivation.
Topics: Blotting, Western; Cell Line, Tumor; Cell Survival; Checkpoint Kinase 1; Comet Assay; DNA; DNA Breaks, Double-Stranded; DNA Damage; DNA Repair; DNA Replication; DNA-Binding Proteins; Endodeoxyribonucleases; Endonucleases; Enzyme Activation; Enzyme Inhibitors; Humans; Nucleic Acid Conformation; Protein Kinases; RNA Interference; S Phase; Thiophenes; Urea | 2011 |
Cytokinetically quiescent (G0/G1) human multiple myeloma cells are susceptible to simultaneous inhibition of Chk1 and MEK1/2.
Topics: Apoptosis; Benzimidazoles; Cell Line, Tumor; Checkpoint Kinase 1; DNA Damage; G1 Phase; Humans; Interleukin-6; MAP Kinase Kinase 1; MAP Kinase Kinase 2; Multiple Myeloma; Protein Kinase Inhibitors; Protein Kinases; Resting Phase, Cell Cycle; Syndecan-1; Thiophenes; Urea | 2011 |
Chk2 deficiency in Myc overexpressing lymphoma cells elicits a synergistic lethal response in combination with PARP inhibition.
Topics: Animals; Apoptosis; Cell Line; Checkpoint Kinase 2; DNA Damage; Fluorescent Antibody Technique; Humans; Lentivirus; Lymphoma; Mice; Mice, Inbred C57BL; Mice, Mutant Strains; NIH 3T3 Cells; Poly (ADP-Ribose) Polymerase-1; Poly(ADP-ribose) Polymerase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins c-myc; Retroviridae; Reverse Transcriptase Polymerase Chain Reaction; Survival Analysis; Thiophenes; Transfection; Urea | 2011 |
Role of checkpoint kinase 1 (Chk1) in the mechanisms of resistance to histone deacetylase inhibitors.
Topics: Animals; Cell Line, Tumor; Cell Survival; Cells, Cultured; Checkpoint Kinase 1; DNA Damage; Drug Resistance; Fibroblasts; Foreskin; Histone Deacetylase Inhibitors; Histones; Humans; Hydroxamic Acids; Immunoblotting; Male; Mice; Protein Kinases; Quinolines; Quinuclidines; RNA Interference; Spleen; Staurosporine; Thiophenes; Urea; Vorinostat | 2011 |
Selective radiosensitization of p53 mutant pancreatic cancer cells by combined inhibition of Chk1 and PARP1.
Topics: Analysis of Variance; Cell Cycle Checkpoints; Checkpoint Kinase 1; DNA Repair; Drug Combinations; Flow Cytometry; Histones; Humans; Immunoblotting; Intestinal Mucosa; Mutation; Pancreatic Neoplasms; Phthalazines; Piperazines; Poly (ADP-Ribose) Polymerase-1; Poly(ADP-ribose) Polymerase Inhibitors; Protein Kinases; Radiation Tolerance; Radiation-Sensitizing Agents; Thiophenes; Tumor Suppressor Protein p53; Urea | 2011 |
Potentiation of the novel topoisomerase I inhibitor indenoisoquinoline LMP-400 by the cell checkpoint and Chk1-Chk2 inhibitor AZD7762.
Topics: Antineoplastic Combined Chemotherapy Protocols; Benzodioxoles; Checkpoint Kinase 1; Checkpoint Kinase 2; Colonic Neoplasms; DNA Replication; Drug Synergism; HT29 Cells; Humans; Isoquinolines; Protein Kinase Inhibitors; Protein Kinases; Protein Serine-Threonine Kinases; Thiophenes; Topoisomerase I Inhibitors; Urea | 2012 |
Evaluation of checkpoint kinase targeting therapy in acute myeloid leukemia with complex karyotype.
Topics: Aged; Apoptosis; Cell Cycle Checkpoints; Cell Line, Tumor; Checkpoint Kinase 1; Humans; Karyotype; Leukemia, Myeloid, Acute; Middle Aged; Molecular Targeted Therapy; Protein Kinase Inhibitors; Protein Kinases; Thiophenes; Urea | 2012 |
Chk'ing p53-deficient breast cancers.
Topics: Animals; Antineoplastic Agents; Breast Neoplasms; Checkpoint Kinase 1; Female; Humans; Molecular Targeted Therapy; Neoplasm Proteins; Protein Kinase Inhibitors; Protein Kinases; Staurosporine; Thiophenes; Tumor Suppressor Protein p53; Urea | 2012 |
Targeting Chk1 in p53-deficient triple-negative breast cancer is therapeutically beneficial in human-in-mouse tumor models.
Topics: Animals; Antineoplastic Agents; Antineoplastic Agents, Phytogenic; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Breast Neoplasms; Camptothecin; Cell Cycle; Cell Line, Tumor; Checkpoint Kinase 1; DNA Damage; DNA, Neoplasm; Female; Genes, cdc; Genes, erbB-2; Genes, p53; Humans; Irinotecan; Mice; Mice, Inbred NOD; Mice, SCID; Molecular Targeted Therapy; Neoplasm Proteins; Protein Kinase Inhibitors; Protein Kinases; Receptors, Estrogen; Receptors, Progesterone; Staurosporine; Thiophenes; Tumor Suppressor Protein p53; Urea; Xenograft Model Antitumor Assays | 2012 |
Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.
Topics: Animals; Antineoplastic Agents; Binding Sites; Camptothecin; Checkpoint Kinase 1; Crystallography, X-Ray; Deoxycytidine; DNA Damage; Drug Design; Drug Synergism; Gemcitabine; High-Throughput Screening Assays; Irinotecan; Mice; Models, Molecular; Molecular Structure; Protein Kinase Inhibitors; Protein Kinases; Rats; Stereoisomerism; Structure-Activity Relationship; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2012 |
Forced mitotic entry of S-phase cells as a therapeutic strategy induced by inhibition of WEE1.
Topics: Animals; Antineoplastic Agents; Apoptosis; Breast Neoplasms; Cell Cycle Proteins; Cell Line; Cell Line, Tumor; Checkpoint Kinase 1; Cyclins; Deoxycytidine; DNA-Binding Proteins; Enhancer of Zeste Homolog 2 Protein; Female; Gemcitabine; Gene Expression Regulation, Neoplastic; Humans; Mice; Mice, SCID; Mitosis; Nuclear Proteins; Polycomb Repressive Complex 2; Protein Kinase Inhibitors; Protein Kinases; Protein-Tyrosine Kinases; Pyrazoles; Pyrimidines; Pyrimidinones; Quinolines; S Phase; Thiazoles; Thiophenes; Transcription Factors; Tumor Burden; Tumor Suppressor Protein p53; Urea; Xenograft Model Antitumor Assays | 2012 |
The checkpoint kinase inhibitor AZD7762 potentiates chemotherapy-induced apoptosis of p53-mutated multiple myeloma cells.
Topics: Antineoplastic Agents; Apoptosis; Cell Cycle; Cell Line, Tumor; Checkpoint Kinase 1; Drug Synergism; Humans; Micronuclei, Chromosome-Defective; Multiple Myeloma; Mutation; Protein Kinase Inhibitors; Protein Kinases; Signal Transduction; Thiophenes; Tumor Suppressor Protein p53; Urea | 2012 |
The Chk1 inhibitor AZD7762 sensitises p53 mutant breast cancer cells to radiation in vitro and in vivo.
Topics: Animals; Apoptosis; Breast Neoplasms; Checkpoint Kinase 1; DNA Damage; Female; G2 Phase Cell Cycle Checkpoints; Gamma Rays; Humans; M Phase Cell Cycle Checkpoints; MCF-7 Cells; Mice; Mice, Nude; Mutation; Protein Kinase Inhibitors; Protein Kinases; Radiation-Sensitizing Agents; Thiophenes; Transplantation, Heterologous; Tumor Suppressor Protein p53; Urea | 2012 |
A kinome screen identifies checkpoint kinase 1 (CHK1) as a sensitizer for RRM1-dependent gemcitabine efficacy.
Topics: Animals; Cattle; Cell Line, Tumor; Cell Survival; Checkpoint Kinase 1; Deoxycytidine; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Gemcitabine; Gene Expression Regulation, Neoplastic; Gene Knockdown Techniques; Humans; Phosphorylation; Protein Binding; Protein Kinase Inhibitors; Protein Kinases; Ribonucleoside Diphosphate Reductase; RNA, Messenger; Small Molecule Libraries; Thiophenes; Treatment Outcome; Tumor Suppressor Proteins; Urea | 2013 |
Chk1/2 inhibition overcomes the cisplatin resistance of head and neck cancer cells secondary to the loss of functional p53.
Topics: Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Squamous Cell; Cell Line, Tumor; Cellular Senescence; Checkpoint Kinase 1; Checkpoint Kinase 2; Cisplatin; DNA Damage; Drug Resistance, Neoplasm; Head and Neck Neoplasms; Humans; Mitosis; Molecular Targeted Therapy; Mutation; Protein Kinase Inhibitors; Protein Kinases; Signal Transduction; Thiophenes; Tumor Suppressor Protein p53; Urea | 2013 |
Checkpoint kinase inhibitor AZD7762 overcomes cisplatin resistance in clear cell carcinoma of the ovary.
Topics: Adenocarcinoma, Clear Cell; Animals; Antineoplastic Agents; Cell Line, Tumor; Cisplatin; Drug Resistance, Neoplasm; Drug Synergism; Female; Mice; Mice, Nude; Ovarian Neoplasms; Protein Kinase Inhibitors; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2014 |
Checkpoint kinase 1 protein expression indicates sensitization to therapy by checkpoint kinase 1 inhibition in non-small cell lung cancer.
Topics: Adenocarcinoma; Antimetabolites, Antineoplastic; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Large Cell; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Cell Survival; Checkpoint Kinase 1; Deoxycytidine; Drug Resistance, Neoplasm; Gemcitabine; Glutamates; Guanine; Humans; Lung Neoplasms; Pemetrexed; Protein Kinase Inhibitors; Protein Kinases; Thiophenes; Urea | 2014 |
Targeting poly(ADP-ribose) polymerase and the c-Myb-regulated DNA damage response pathway in castration-resistant prostate cancer.
Topics: Animals; BRCA1 Protein; Carrier Proteins; Castration; Cell Cycle Checkpoints; DNA Damage; DNA-Binding Proteins; Humans; Male; Mice; Mice, Nude; Nuclear Proteins; Phthalazines; Piperazines; Poly(ADP-ribose) Polymerase Inhibitors; Poly(ADP-ribose) Polymerases; Prostatic Neoplasms; Proto-Oncogene Proteins c-myb; Receptors, Androgen; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2014 |
Effects of the small-molecule inhibitor of integrin α4, TBC3486, on pre-B-ALL cells.
Topics: Animals; Antineoplastic Agents; Coculture Techniques; Drug Resistance, Neoplasm; Humans; Inflammation; Integrin alpha4; Leukemia; Mice; Neoplasm Transplantation; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Precursor Cells, B-Lymphoid; Stromal Cells; Thiophenes; Urea | 2014 |
Association between cellular radiosensitivity and G1/G2 checkpoint proficiencies in human cholangiocarcinoma cell lines.
Topics: Bile Duct Neoplasms; Bile Ducts, Intrahepatic; Cell Line, Tumor; Cholangiocarcinoma; Dose-Response Relationship, Radiation; G1 Phase Cell Cycle Checkpoints; G2 Phase Cell Cycle Checkpoints; Gene Expression Regulation, Neoplastic; Humans; Radiation Tolerance; Thiophenes; Tumor Suppressor Protein p53; Urea | 2014 |
Chk1 inhibition as a novel therapeutic strategy for treating triple-negative breast and ovarian cancers.
Topics: Benzodiazepinones; Biomarkers, Tumor; Cell Line, Tumor; Checkpoint Kinase 1; Cisplatin; Deoxycytidine; Drug Synergism; Female; Gemcitabine; Gene Expression Regulation, Neoplastic; HT29 Cells; Humans; Indoles; MCF-7 Cells; Ovarian Neoplasms; Protein Kinase Inhibitors; Protein Kinases; Pyrazoles; Pyridones; Thiophenes; Triple Negative Breast Neoplasms; Urea | 2014 |
ATR inhibition preferentially targets homologous recombination-deficient tumor cells.
Topics: Antineoplastic Agents; Ataxia Telangiectasia Mutated Proteins; Cell Survival; Checkpoint Kinase 1; Drug Resistance, Neoplasm; HeLa Cells; Homologous Recombination; Humans; MCF-7 Cells; Molecular Targeted Therapy; Neoplasms; Protein Kinases; Pyrazines; Signal Transduction; Sulfones; Thiophenes; Urea | 2015 |
Pharmacological targeting the ATR-CHK1-WEE1 axis involves balancing cell growth stimulation and apoptosis.
Topics: Apoptosis; Ataxia Telangiectasia Mutated Proteins; Blotting, Western; Carcinoma, Non-Small-Cell Lung; Cell Cycle; Cell Cycle Proteins; Cell Proliferation; Checkpoint Kinase 1; Flow Cytometry; Humans; Immunoenzyme Techniques; Lung Neoplasms; Mitosis; Nuclear Proteins; Protein Kinases; Protein-Tyrosine Kinases; Pyrazoles; Pyrimidines; Pyrimidinones; Thiophenes; Tumor Cells, Cultured; Urea | 2014 |
Combined CDKN1A/TP53 mutation in bladder cancer is a therapeutic target.
Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Benzodiazepinones; Cell Cycle; Cell Line, Tumor; Checkpoint Kinase 1; Cyclin-Dependent Kinase Inhibitor p21; Deoxycytidine; Drug Synergism; Gemcitabine; Humans; Mice; Mutation; Protein Kinases; Pyrazoles; Thiophenes; Tumor Suppressor Protein p53; Urea; Urinary Bladder Neoplasms; Xenograft Model Antitumor Assays | 2015 |
Synthesis and SAR of thieno[3,2-b]pyridinyl urea derivatives as urotensin-II receptor antagonists.
Topics: Animals; ERG1 Potassium Channel; Ether-A-Go-Go Potassium Channels; Humans; Microsomes, Liver; Protein Binding; Pyridines; Rats; Receptors, G-Protein-Coupled; Structure-Activity Relationship; Thiophenes; Urea | 2014 |
Constitutive activation of the DNA damage response pathway as a novel therapeutic target in diffuse large B-cell lymphoma.
Topics: Antineoplastic Agents; Apoptosis; Benzodiazepinones; cdc25 Phosphatases; Cell Line, Tumor; Cell Proliferation; Checkpoint Kinase 1; Checkpoint Kinase 2; DNA Damage; Dose-Response Relationship, Drug; Histones; Humans; Lymphoma, Large B-Cell, Diffuse; Molecular Targeted Therapy; Phosphorylation; Protein Kinase Inhibitors; Protein Kinases; Proto-Oncogene Proteins c-myc; Pyrazoles; Thiophenes; Time Factors; Tumor Cells, Cultured; Urea | 2015 |
DNA replication stress as an Achilles' heel of cancer.
Topics: Antineoplastic Agents; Benzodiazepinones; Checkpoint Kinase 2; DNA Damage; Humans; Lymphoma, Large B-Cell, Diffuse; Protein Kinase Inhibitors; Protein Kinases; Pyrazoles; Thiophenes; Urea | 2015 |
Aven-mediated checkpoint kinase control regulates proliferation and resistance to chemotherapy in conventional osteosarcoma.
Topics: Adaptor Proteins, Signal Transducing; Antibiotics, Antineoplastic; Apoptosis; Apoptosis Regulatory Proteins; Ataxia Telangiectasia Mutated Proteins; Bone Neoplasms; Cell Line, Tumor; Checkpoint Kinase 1; DNA Damage; Doxorubicin; G2 Phase Cell Cycle Checkpoints; Gene Expression Profiling; Gene Expression Regulation, Neoplastic; Humans; Membrane Proteins; Oligonucleotide Array Sequence Analysis; Osteosarcoma; Phosphorylation; Protein Kinases; RNA Interference; Signal Transduction; Thiophenes; Urea | 2015 |
Exploring the chemical space of ureidothiophene-2-carboxylic acids as inhibitors of the quorum sensing enzyme PqsD from Pseudomonas aeruginosa.
Topics: Bacterial Proteins; Dose-Response Relationship, Drug; Enzyme Inhibitors; Models, Molecular; Molecular Structure; Pseudomonas aeruginosa; Quorum Sensing; Structure-Activity Relationship; Thiophenes; Urea | 2015 |
Enhancement of hypoxia-activated prodrug TH-302 anti-tumor activity by Chk1 inhibition.
Topics: Animals; Antineoplastic Agents; Apoptosis; CDC2 Protein Kinase; Cell Cycle Checkpoints; Cell Survival; Checkpoint Kinase 1; Colonic Neoplasms; DNA Damage; Female; Histones; HT29 Cells; Humans; Mice; Mice, Nude; Mutation; Nitroimidazoles; Phosphoproteins; Phosphoramide Mustards; Phosphorylation; Protein Kinase Inhibitors; Protein Kinases; Rad51 Recombinase; Signal Transduction; Thiophenes; Tumor Suppressor Protein p53; Urea | 2015 |
Pharmacological inactivation of CHK1 and WEE1 induces mitotic catastrophe in nasopharyngeal carcinoma cells.
Topics: Animals; Ataxia Telangiectasia Mutated Proteins; Carcinoma; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Checkpoint Kinase 1; DNA Damage; Flow Cytometry; G2 Phase; Gene Expression Regulation, Neoplastic; Green Fluorescent Proteins; HeLa Cells; Humans; Mice; Mice, Inbred BALB C; Mitosis; Nasopharyngeal Carcinoma; Nasopharyngeal Neoplasms; Neoplasm Invasiveness; Neoplasm Transplantation; Nuclear Proteins; Phosphorylation; Protein Kinase Inhibitors; Protein Kinases; Protein-Tyrosine Kinases; Pyrazoles; Pyrimidines; Pyrimidinones; RNA Interference; Thiophenes; Urea | 2015 |
Combined inhibition of the cell cycle related proteins Wee1 and Chk1/2 induces synergistic anti-cancer effect in melanoma.
Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Cell Cycle Checkpoints; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Checkpoint Kinase 2; Drug Synergism; Humans; Melanoma; Melanoma, Cutaneous Malignant; Mice; Nuclear Proteins; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrazoles; Pyrimidines; Pyrimidinones; Skin Neoplasms; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2015 |
Chemogenetic profiling identifies RAD17 as synthetically lethal with checkpoint kinase inhibition.
Topics: Antineoplastic Agents; Biomarkers, Pharmacological; Cell Cycle; Cell Cycle Proteins; Checkpoint Kinase 1; Checkpoint Kinase 2; DNA Damage; DNA-Binding Proteins; Drug Discovery; HeLa Cells; Humans; Molecular Targeted Therapy; Mutation; Neoplasms; Nuclear Proteins; Protein Kinases; Protein-Tyrosine Kinases; RNA, Small Interfering; Saccharomyces cerevisiae; Saccharomyces cerevisiae Proteins; Thiophenes; Urea | 2015 |
Characterization of a mantle cell lymphoma cell line resistant to the Chk1 inhibitor PF-00477736.
Topics: Antineoplastic Agents; Benzodiazepinones; Cell Cycle; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Checkpoint Kinase 1; Cyclin D1; Dasatinib; Dose-Response Relationship, Drug; Drug Resistance, Neoplasm; Humans; Lymphoma, Mantle-Cell; Molecular Targeted Therapy; Nuclear Proteins; Protein Kinase Inhibitors; Protein Kinases; Protein-Tyrosine Kinases; Pyrazoles; Pyrimidines; Pyrimidinones; Signal Transduction; src-Family Kinases; Thiophenes; Time Factors; Urea | 2015 |
Dissociation of gemcitabine chemosensitization by CHK1 inhibition from cell cycle checkpoint abrogation and aberrant mitotic entry.
Topics: Antimetabolites, Antineoplastic; Cell Cycle Checkpoints; Cell Line, Tumor; Checkpoint Kinase 1; Cyclin B1; Deoxycytidine; DNA Damage; Drug Screening Assays, Antitumor; G2 Phase Cell Cycle Checkpoints; Gemcitabine; Humans; Mitosis; Nocodazole; Pancreatic Neoplasms; Thiophenes; Urea | 2016 |
Preliminary evaluation of prostate-targeted radiotherapy using (131) I-MIP-1095 in combination with radiosensitising chemotherapeutic drugs.
Topics: Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Bortezomib; Cell Line, Tumor; Cell Proliferation; Disulfiram; Glutamates; Humans; Imidazoles; Iodine Radioisotopes; Male; Molecular Targeted Therapy; Phthalazines; Piperazines; Prostate; Spheroids, Cellular; Thiophenes; Topotecan; Tumor Cells, Cultured; Urea | 2016 |
Antiangiogenic 1-Aryl-3-[3-(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas Inhibit MCF-7 and MDA-MB-231 Human Breast Cancer Cell Lines Through PI3K/Akt and MAPK/Erk Pathways.
Topics: Angiogenesis Inhibitors; Apoptosis; Blotting, Western; Breast; Breast Neoplasms; Cell Proliferation; Cells, Cultured; Female; Humans; MAP Kinase Signaling System; Neovascularization, Pathologic; Phenylurea Compounds; Phosphatidylinositol 3-Kinases; Proto-Oncogene Proteins c-akt; Signal Transduction; Thiophenes; Urea | 2016 |
Targeting radioresistant breast cancer cells by single agent CHK1 inhibitor via enhancing replication stress.
Topics: Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Checkpoint Kinase 1; DNA Repair; Homologous Recombination; Humans; MCF-7 Cells; Phenylurea Compounds; Protein Kinase Inhibitors; Pyrazines; Radiation Tolerance; Radiation-Sensitizing Agents; Thiophenes; Urea | 2016 |
Birinapant (TL32711) Improves Responses to GEM/AZD7762 Combination Therapy in Triple-negative Breast Cancer Cell Lines.
Topics: Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Cell Line, Tumor; Checkpoint Kinase 1; Deoxycytidine; Dipeptides; DNA Repair; Female; Gemcitabine; Humans; Indoles; Phosphorylation; Thiophenes; Triple Negative Breast Neoplasms; Urea | 2016 |
Checkpoint kinase 1 expression is an adverse prognostic marker and therapeutic target in MYC-driven medulloblastoma.
Topics: Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Benzodiazepinones; Biomarkers, Tumor; Cell Survival; Cerebellar Neoplasms; Checkpoint Kinase 1; Cisplatin; Disease-Free Survival; Genes, myc; Humans; Kaplan-Meier Estimate; Medulloblastoma; Prognosis; Pyrazoles; Thiophenes; Urea | 2016 |
Structure-based discovery of opioid analgesics with reduced side effects.
Topics: Analgesia; Analgesics, Opioid; Animals; Drug Discovery; GTP-Binding Protein alpha Subunits, Gi-Go; HEK293 Cells; Humans; Male; Mice; Mice, Inbred C57BL; Mice, Knockout; Molecular Docking Simulation; Pain; Receptors, Opioid, mu; Spiro Compounds; Structure-Activity Relationship; Thiophenes; Urea | 2016 |
Suppression of the metastatic spread of breast cancer by DN10764 (AZD7762)-mediated inhibition of AXL signaling.
Topics: A549 Cells; Adenocarcinoma; Animals; Antineoplastic Agents; Apoptosis; Axl Receptor Tyrosine Kinase; Breast Neoplasms; Caspase 3; Caspase 7; Cell Movement; Cell Proliferation; Dose-Response Relationship, Drug; Female; Human Umbilical Vein Endothelial Cells; Humans; Intercellular Signaling Peptides and Proteins; Lung Neoplasms; Mice, Inbred BALB C; Mice, Nude; Neovascularization, Physiologic; Protein Kinase Inhibitors; Proto-Oncogene Proteins; Receptor Protein-Tyrosine Kinases; RNA Interference; Signal Transduction; Thiophenes; Time Factors; Transfection; Tumor Burden; Urea; Xenograft Model Antitumor Assays | 2016 |
MEK inhibitors block growth of lung tumours with mutations in ataxia-telangiectasia mutated.
Topics: Animals; Ataxia Telangiectasia Mutated Proteins; Benzamides; Cell Line, Tumor; Cell Proliferation; Diphenylamine; Humans; Lung Neoplasms; Mice, Nude; Mutation; Protein Kinase Inhibitors; Proto-Oncogene Proteins B-raf; Pyridones; Pyrimidinones; ras Proteins; RNA Interference; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2016 |
Inhibition of CHK1 and WEE1 as a new therapeutic approach in diffuse large B cell lymphomas with MYC deregulation.
Topics: Cell Cycle Proteins; Cell Line; Checkpoint Kinase 1; Female; Humans; Lymphoma, Large B-Cell, Diffuse; Male; Nuclear Proteins; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Proto-Oncogene Proteins c-myc; Pyrazoles; Pyrimidines; Pyrimidinones; Thiophenes; Urea | 2018 |
Combined inhibition of Wee1 and Chk1 gives synergistic DNA damage in S-phase due to distinct regulation of CDK activity and CDC45 loading.
Topics: A549 Cells; Cell Cycle Proteins; Cell Line, Tumor; Checkpoint Kinase 1; Cyclin-Dependent Kinases; DNA Damage; DNA Replication; Drug Synergism; Flow Cytometry; Humans; Nuclear Proteins; Phenylurea Compounds; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrazines; Pyrazoles; Pyrimidines; Pyrimidinones; S Phase; Thiophenes; Urea | 2017 |
Checkpoint kinase inhibitor AZD7762 strongly sensitises urothelial carcinoma cells to gemcitabine.
Topics: Antimetabolites, Antineoplastic; Carcinoma, Transitional Cell; Caspases; Cell Cycle; Cell Line, Tumor; Cell Survival; Checkpoint Kinase 1; Checkpoint Kinase 2; Deoxycytidine; DNA Damage; Drug Screening Assays, Antitumor; Drug Synergism; Gemcitabine; Gene Expression Regulation, Neoplastic; Humans; Poly(ADP-ribose) Polymerases; Protein Kinase Inhibitors; RNA, Small Interfering; Thiophenes; Urea; Urinary Bladder Neoplasms | 2017 |
HPLC-UV method for simultaneous determination of MK-1775 and AZD-7762 in both acetonitrile-aqueous solution and mouse plasma.
Topics: Animals; Chromatography, High Pressure Liquid; Female; Limit of Detection; Linear Models; Mice; Mice, Inbred BALB C; Pyrazoles; Pyrimidines; Pyrimidinones; Reproducibility of Results; Solid Phase Extraction; Spectrophotometry, Ultraviolet; Thiophenes; Urea | 2017 |
Mutations of the LIM protein AJUBA mediate sensitivity of head and neck squamous cell carcinoma to treatment with cell-cycle inhibitors.
Topics: Animals; Antineoplastic Agents; Apoptosis; Carcinoma, Squamous Cell; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Checkpoint Kinase 1; Checkpoint Kinase 2; Dose-Response Relationship, Drug; G2 Phase Cell Cycle Checkpoints; Genotype; Head and Neck Neoplasms; Humans; LIM Domain Proteins; Mice, Nude; Molecular Targeted Therapy; Mutation; Nuclear Proteins; Phenotype; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Protein-Tyrosine Kinases; Proto-Oncogene Proteins; Pteridines; Pyrazoles; Pyrimidines; Pyrimidinones; ras Proteins; RNA Interference; Signal Transduction; Smad4 Protein; Squamous Cell Carcinoma of Head and Neck; Thiophenes; Time Factors; Transfection; Tumor Burden; Urea; Xenograft Model Antitumor Assays | 2017 |
Prolonged Activation of the Htr2b Serotonin Receptor Impairs Glucose Stimulated Insulin Secretion and Mitochondrial Function in MIN6 Cells.
Topics: Adenosine Triphosphate; Animals; Cell Line; Gene Expression Regulation; Glucose; Humans; Indoles; Insulin; Insulin-Secreting Cells; Islets of Langerhans; Mice; Mitochondria; Oxygen Consumption; Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha; PPAR gamma; Receptors, Serotonin; Serotonin; Thiophenes; Urea | 2017 |
Targeting DNA Damage Response in Prostate Cancer by Inhibiting Androgen Receptor-CDC6-ATR-Chk1 Signaling.
Topics: Androgen Receptor Antagonists; Animals; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Biomarkers; Cell Cycle Checkpoints; Cell Cycle Proteins; Cell Line, Tumor; Checkpoint Kinase 1; DNA Damage; DNA Replication; DNA-Binding Proteins; Humans; Male; Mice; Mice, Nude; Nuclear Proteins; Phosphorylation; Prostatic Neoplasms; Receptors, Androgen; Signal Transduction; Thiophenes; Urea | 2017 |
Feedback regulation of methyl methanesulfonate and ultraviolet-sensitive gene clone 81 via ATM/Chk2 pathway contributes to the resistance of MCF-7 breast cancer cells to cisplatin.
Topics: Antineoplastic Agents; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Breast Neoplasms; Checkpoint Kinase 2; Cisplatin; DNA-Binding Proteins; Drug Resistance, Neoplasm; Endonucleases; Feedback; Female; Gene Knockdown Techniques; Humans; MCF-7 Cells; Morpholines; Protein Kinase Inhibitors; Pyrones; Signal Transduction; Thiophenes; Urea | 2017 |
Role of CPS1 in Cell Growth, Metabolism and Prognosis in LKB1-Inactivated Lung Adenocarcinoma.
Topics: Adenocarcinoma; Aged; AMP-Activated Protein Kinase Kinases; Carbamoyl-Phosphate Synthase (Ammonia); Carcinoma, Squamous Cell; Cell Line, Tumor; Cell Proliferation; Deoxycytidine; Female; Gemcitabine; Gene Knockdown Techniques; Humans; Kaplan-Meier Estimate; Lung Neoplasms; Male; Metabolic Networks and Pathways; Metabolome; Middle Aged; Pemetrexed; Prognosis; Proportional Hazards Models; Protein Serine-Threonine Kinases; Proteome; RNA, Messenger; Signal Transduction; Survival Rate; Thiophenes; Tissue Array Analysis; Urea | 2017 |
Construction of ferrocene modified conducting polymer based amperometric urea biosensor.
Topics: Aniline Compounds; Biosensing Techniques; Electric Conductivity; Electrochemical Techniques; Enzymes, Immobilized; Ferrous Compounds; Humans; Metallocenes; Polymers; Pyrroles; Thiophenes; Urea; Urease | 2017 |
Gemcitabine and Chk1 Inhibitor AZD7762 Synergistically Suppress the Growth of Lkb1-Deficient Lung Adenocarcinoma.
Topics: Adenocarcinoma; AMP-Activated Protein Kinase Kinases; Animals; Antimetabolites, Antineoplastic; Apoptosis; Biomarkers, Tumor; Carcinoma, Non-Small-Cell Lung; Cell Proliferation; Checkpoint Kinase 1; Deoxycytidine; Drug Synergism; Drug Therapy, Combination; Female; Gemcitabine; Humans; Lung Neoplasms; Mice; Mice, Knockout; Mice, Nude; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins p21(ras); Thiophenes; Tumor Cells, Cultured; Tumor Suppressor Protein p53; Urea; Xenograft Model Antitumor Assays | 2017 |
Phenotypic Optimization of Urea-Thiophene Carboxamides To Yield Potent, Well Tolerated, and Orally Active Protective Agents against Aminoglycoside-Induced Hearing Loss.
Topics: Administration, Oral; Aminoglycosides; Animals; Drug Evaluation, Preclinical; Hearing Loss; Rats; Safety; Structure-Activity Relationship; Thiophenes; Urea; Zebrafish | 2018 |
Chk1 inhibitors overcome imatinib resistance in chronic myeloid leukemia cells.
Topics: Animals; Apoptosis; Cell Line, Tumor; Cell Proliferation; Checkpoint Kinase 1; Drug Resistance, Neoplasm; Fusion Proteins, bcr-abl; Humans; Imatinib Mesylate; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Mice; Mice, Inbred BALB C; Pyrazoles; Pyrimidines; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2018 |
Acetyl-macrocalin B, an ent-kaurane diterpenoid, initiates apoptosis through the ROS-p38-caspase 9-dependent pathway and induces G2/M phase arrest via the Chk1/2-Cdc25C-Cdc2/cyclin B axis in non-small cell lung cancer.
Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Carcinoma, Non-Small-Cell Lung; Caspase 9; Cell Cycle Proteins; Cell Line, Tumor; Diterpenes; Drug Synergism; Female; G2 Phase Cell Cycle Checkpoints; Humans; Lamiaceae; Lung Neoplasms; Mice; Mice, Nude; Mitogen-Activated Protein Kinase 14; Reactive Oxygen Species; Signal Transduction; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2018 |
The novel μ-opioid receptor agonist PZM21 depresses respiration and induces tolerance to antinociception.
Topics: Analgesics, Opioid; Animals; Depression; Drug Tolerance; Male; Mice; Mice, Inbred C57BL; Receptors, Opioid, mu; Thiophenes; Urea | 2018 |
DUOXA1-mediated ROS production promotes cisplatin resistance by activating ATR-Chk1 pathway in ovarian cancer.
Topics: Aged; Animals; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Benzodiazepinones; Cell Line, Tumor; Checkpoint Kinase 1; Cisplatin; Drug Resistance, Neoplasm; Female; Humans; Kaplan-Meier Estimate; Membrane Proteins; Mice; Mice, Nude; Middle Aged; Ovarian Neoplasms; Prognosis; Pyrazoles; Reactive Oxygen Species; Signal Transduction; Thiophenes; Urea; Xenograft Model Antitumor Assays | 2018 |
Multiple DNA damage-dependent and DNA damage-independent stress responses define the outcome of ATR/Chk1 targeting in medulloblastoma cells.
Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Caenorhabditis elegans; Cell Line, Tumor; Checkpoint Kinase 1; Cisplatin; DNA Damage; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Drug Synergism; Hedgehog Proteins; Humans; Medulloblastoma; Neurons; Primary Cell Culture; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-myc; Rats; Rats, Wistar; RNA, Small Interfering; Signal Transduction; Thiophenes; Toxicity Tests; Urea | 2018 |
Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor.
Topics: Allosteric Regulation; Allosteric Site; Biosensing Techniques; Biotin; Humans; Interferometry; Ligands; Loperamide; Methadone; Protein Binding; Receptors, Opioid, mu; Sensitivity and Specificity; Single-Domain Antibodies; Small Molecule Libraries; Solutions; Streptavidin; Thiophenes; Urea | 2018 |
Effects of a checkpoint kinase inhibitor, AZD7762, on tumor suppression and bone remodeling.
Topics: Animals; Bioprinting; Bone and Bones; Bone Remodeling; Calcification, Physiologic; Carbazoles; Cell Culture Techniques; Cell Differentiation; Cell Line, Tumor; Cell Proliferation; Checkpoint Kinase 1; Checkpoint Kinase 2; Down-Regulation; Drug Screening Assays, Antitumor; Humans; Mice; Neoplasms; Osteoblasts; Osteoclasts; Osteogenesis; Printing, Three-Dimensional; Protein Kinase Inhibitors; RAW 264.7 Cells; Spheroids, Cellular; Thiophenes; Tumor Suppressor Protein p53; Urea; X-Ray Microtomography | 2018 |
Extending Remission and Reversing New-Onset Type 1 Diabetes by Targeted Ablation of Autoreactive T Cells.
Topics: Animals; Diabetes Mellitus, Type 1; Enzyme Inhibitors; Imidazoles; Mice; Mice, Inbred NOD; Pancreas; Piperazines; Pyrazoles; Pyrimidines; Pyrimidinones; T-Lymphocytes; Thiophenes; Urea | 2018 |
Mu-opioid Receptor (MOR) Biased Agonists Induce Biphasic Dose-dependent Hyperalgesia and Analgesia, and Hyperalgesic Priming in the Rat.
Topics: Analgesics, Opioid; Animals; Dinoprostone; Dose-Response Relationship, Drug; Hyperalgesia; Injections, Intradermal; Male; Nociception; Pain Threshold; Rats, Sprague-Dawley; Receptors, Opioid, mu; Spiro Compounds; Thiophenes; Urea | 2018 |
Acetyl-macrocalin B suppresses tumor growth in esophageal squamous cell carcinoma and exhibits synergistic anti-cancer effects with the Chk1/2 inhibitor AZD7762.
Topics: Animals; Antineoplastic Agents, Phytogenic; Antineoplastic Combined Chemotherapy Protocols; Cell Line, Tumor; Cell Proliferation; Checkpoint Kinase 1; Checkpoint Kinase 2; Diterpenes, Kaurane; Drug Synergism; Esophageal Neoplasms; Esophageal Squamous Cell Carcinoma; Female; G2 Phase Cell Cycle Checkpoints; Humans; Mice, Inbred BALB C; Mice, Nude; p38 Mitogen-Activated Protein Kinases; Phosphorylation; Protein Kinase Inhibitors; Reactive Oxygen Species; Signal Transduction; Thiophenes; Tumor Burden; Urea; Xenograft Model Antitumor Assays | 2019 |
Synthesis of urea analogues bearing N-alkyl-N'-(thiophen-2-yl) scaffold and evaluation of their innate immune response to toll-like receptors.
Topics: Cell Line; Cell Survival; Dose-Response Relationship, Drug; Humans; Molecular Docking Simulation; Molecular Structure; Structure-Activity Relationship; Thiophenes; Toll-Like Receptors; Urea | 2019 |
Fbxo6 confers drug-sensitization to cisplatin via inhibiting the activation of Chk1 in non-small cell lung cancer.
Topics: A549 Cells; Aged; Aged, 80 and over; Apoptosis; Carcinoma, Non-Small-Cell Lung; Cell Proliferation; Checkpoint Kinase 1; Cisplatin; Drug Resistance, Neoplasm; Enzyme Activation; Female; Gene Knockdown Techniques; Humans; Lung Neoplasms; Male; Neoplasm Staging; Prognosis; SKP Cullin F-Box Protein Ligases; Thiophenes; Urea | 2019 |
Functional characterization of a novel opioid, PZM21, and its effects on the behavioural responses to morphine.
Topics: Analgesics, Opioid; Animals; Behavior, Animal; Dose-Response Relationship, Drug; Drug Delivery Systems; Injections, Intravenous; Injections, Spinal; Locomotion; Male; Mice; Mice, Inbred C57BL; Morphine; Rats; Rats, Sprague-Dawley; Rats, Wistar; Structure-Activity Relationship; Thiophenes; Urea | 2019 |
ORC-13661 protects sensory hair cells from aminoglycoside and cisplatin ototoxicity.
Topics: Amikacin; Aminoglycosides; Animals; Anti-Bacterial Agents; Antineoplastic Agents; Cell Culture Techniques; Cells, Cultured; Cisplatin; Disease Models, Animal; Dose-Response Relationship, Drug; Hair Cells, Auditory; Humans; Intravital Microscopy; Ion Channels; Male; Mechanotransduction, Cellular; Mice; Ototoxicity; Patch-Clamp Techniques; Protective Agents; Rats; Thiophenes; Time-Lapse Imaging; Urea; Zebrafish | 2019 |
Targeting AXL and the DNA Damage Response Pathway as a Novel Therapeutic Strategy in Melanoma.
Topics: Animals; Apoptosis; Axl Receptor Tyrosine Kinase; Biomarkers, Tumor; Cell Cycle Checkpoints; Cell Proliferation; Checkpoint Kinase 1; Checkpoint Kinase 2; DNA Damage; DNA Repair; Drug Resistance, Neoplasm; Drug Therapy, Combination; Female; Gene Expression Regulation, Neoplastic; Humans; Lymphatic Metastasis; Melanoma; Mice; Mice, Nude; Neoplasm Invasiveness; Proto-Oncogene Proteins; Receptor Protein-Tyrosine Kinases; RNA, Small Interfering; Thiophenes; Tumor Cells, Cultured; Urea; Xenograft Model Antitumor Assays | 2020 |
Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists.
Topics: Benzimidazoles; beta-Arrestins; HEK293 Cells; Humans; Piperidines; Receptors, Opioid, mu; Spiro Compounds; Thiophenes; Urea | 2020 |
Combination of CHEK1/2 inhibition and ionizing radiation results in abscopal tumor response through increased micronuclei formation.
Topics: Animals; Cell Line, Tumor; Cell Nucleus; Checkpoint Kinase 1; Checkpoint Kinase 2; Female; G2 Phase Cell Cycle Checkpoints; Humans; Interferon-beta; Melanoma, Experimental; Membrane Proteins; Mice, Inbred C57BL; Micronucleus Tests; Neoplasm Proteins; RNA Interference; RNA, Small Interfering; STAT1 Transcription Factor; Thiophenes; Tumor Burden; Urea; Xenograft Model Antitumor Assays | 2020 |
Molecular Dynamics Simulations to Investigate How PZM21 Affects the Conformational State of the μ-Opioid Receptor Upon Activation.
Topics: Analgesia; Analgesics, Opioid; Animals; Dose-Response Relationship, Drug; GTP-Binding Proteins; Humans; Ligands; Molecular Dynamics Simulation; Morphine; Pain; Receptors, Opioid, mu; Spiro Compounds; Thiophenes; Urea | 2020 |
Antinociceptive, reinforcing, and pruritic effects of the G-protein signalling-biased mu opioid receptor agonist PZM21 in non-human primates.
Topics: Analgesics; Animals; Dose-Response Relationship, Drug; Female; Macaca mulatta; Male; Pruritus; Receptors, Opioid, mu; Reinforcement, Psychology; Thiophenes; Urea | 2020 |
Radiosensitization of NSCLC cells to X-rays and carbon ions by the CHK1/CHK2 inhibitor AZD7762, Honokiol and Tunicamycin.
Topics: Antineoplastic Agents; Apoptosis; Biphenyl Compounds; Carbon; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Cell Proliferation; Checkpoint Kinase 1; Checkpoint Kinase 2; DNA Breaks, Double-Stranded; G2 Phase Cell Cycle Checkpoints; Humans; Ions; Lignans; Linear Energy Transfer; Lung Neoplasms; Protein Kinase Inhibitors; Radiation Tolerance; Radiation-Sensitizing Agents; Thiophenes; Tunicamycin; Urea; X-Rays | 2020 |
Temozolomide and AZD7762 Induce Synergistic Cytotoxicity Effects on Human Glioma Cells.
Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Survival; Dose-Response Relationship, Drug; Drug Synergism; Gene Expression Regulation, Neoplastic; Glioma; Humans; Temozolomide; Thiophenes; Urea | 2020 |
Molecular Modeling of µ Opioid Receptor Ligands with Various Functional Properties: PZM21, SR-17018, Morphine, and Fentanyl-Simulated Interaction Patterns Confronted with Experimental Data.
Topics: Animals; Fentanyl; Humans; Molecular Dynamics Simulation; Morphine; Receptors, Opioid; Thiophenes; Urea | 2020 |
Crystal Structure of the Kinase Domain of MerTK in Complex with AZD7762 Provides Clues for Structure-Based Drug Development.
Topics: A549 Cells; c-Mer Tyrosine Kinase; Cell Line, Tumor; Crystallography, X-Ray; Down-Regulation; Drug Screening Assays, Antitumor; Gene Expression Regulation, Neoplastic; Humans; Lung Neoplasms; Models, Molecular; Phosphorylation; Protein Binding; Protein Conformation; Protein Domains; Structure-Activity Relationship; Thiophenes; Urea | 2020 |
Probing biased activation of mu-opioid receptor by the biased agonist PZM21 using all atom molecular dynamics simulation.
Topics: Allosteric Regulation; Animals; Aspartic Acid; Cluster Analysis; Conserved Sequence; Crystallization; Humans; Ligands; Mice; Molecular Dynamics Simulation; Morphine; Principal Component Analysis; Protein Conformation; Receptors, Opioid, mu; Signal Transduction; Structural Homology, Protein; Thiophenes; Tyrosine; Urea; Water | 2021 |
Thiophen urea derivatives as a new class of hepatitis C virus entry inhibitors.
Topics: Antiviral Agents; Dose-Response Relationship, Drug; Hepacivirus; Microbial Sensitivity Tests; Molecular Docking Simulation; Molecular Structure; Structure-Activity Relationship; Thiophenes; Urea; Viral Envelope Proteins; Virus Internalization | 2021 |
Novel tetrahydrobenzo[b]thiophen-2-yl)urea derivatives as novel α-glucosidase inhibitors: Synthesis, kinetics study, molecular docking, and in vivo anti-hyperglycemic evaluation.
Topics: alpha-Glucosidases; Animals; Blood Glucose; Cell Line; Dose-Response Relationship, Drug; Glucose Tolerance Test; Glycoside Hydrolase Inhibitors; Humans; Hypoglycemic Agents; Kinetics; Molecular Docking Simulation; Molecular Structure; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Thiophenes; Urea | 2021 |