Page last updated: 2024-08-18

thiophenes and pyrimidinones

thiophenes has been researched along with pyrimidinones in 139 studies

Research

Studies (139)

Timeframe	Studies, this research(%)	All Research%
pre-1990	4 (2.88)	18.7374
1990's	14 (10.07)	18.2507
2000's	21 (15.11)	29.6817
2010's	77 (55.40)	24.3611
2020's	23 (16.55)	2.80

Authors

Authors	Studies
Sauter, F; Schrom, E; Stanetty, P	1
Devani, MB; Padhya, AC; Parikh, SH; Pathak, US; Shah, GF; Shishoo, CJ	1
Aboulwafa, OM; Ismail, KA; Koreish, EA	1
Russo, F; Santagati, NA; Spampinato, S; Venturini, R	1
Amico-Roxas, M; Bousquet, E; Caruso, A; Guerrera, F; Romeo, G	1
Amin, SG; Manhas, MS; Sharma, SD	1
Belvisi, L; Caliari, S; Canevotti, R; Cirillo, R; Fici, F; Paleari, F; Poma, D; Renzetti, AR; Salimbeni, A; Subissi, A	1
Ciccocioppo, R; Cirillo, R; Massi, M; Polidori, C; Pompei, P	2
Caliari, S; Castellucci, A; Cirillo, R; Cucchi, P; Evangelista, S; Giachetti, A; Guelfi, M; Renzetti, AR; Salimbeni, A; Subissi, A	1
Caruso, A; Cutuli, V; Modica, M; Santagati, A; Santagati, M	1
Catalioto, RM; Criscuoli, M; Giachetti, A; Porchia, R; Renzetti, AR; Subissi, A	1
Criscuoli, M; Renzetti, AR; Salimbeni, A; Subissi, A	1
Caccamo, F; Caruso, A; Cutuli, VM; Santagati, NA	1
Brunner, HR; Capone, P; Del Re, G; Noël, B; Nussberger, J	1
Manjunath, KS; Mohan, S; Naragund, LV; Shishoo, CJ	1
Algueró, M; Bartroli, J; Boncompte, E; Conte, L; Forn, J; García-Rafanell, J; Merlos, M; Ramis, J; Turmo, E; Vericat, ML	1
Shinkwin, AE; Threadgill, MD; Whish, WJ	1
Cagnotto, A; Goegan, M; Mennini, T; Modica, M; Russo, F; Santagati, A; Santagati, M	1
Dransfield, DT; Hagos, A; Januszczyk, P; Seley, KL; Zhang, L	1
Fulston, M; Houge-Frydrych, CS; Jones, JJ; Stefanska, AL; Warr, SR	1
Bousquet, E; Prezzavento, O; Ronsisvalle, G; Santagati, NA; Spampinato, S	1
Chen, C; Chen, Y; Guo, Z; Saunders, J; Struthers, RS; Wu, D; Xie, Q; Zhu, YF	1
Barzaghi, M; Destro, R; Lo Presti, L; Soave, R	1
Basso, G; Disarò, S; Fortunato, E; Queiroz, MJ; Salvador, A; Vedaldi, D; Viola, G	1
Hariguchi, N; Hirai, S; Horoiwa, S; Kasahara, R; Kikuchi, H; Matsumoto, M; Oshima, Y; Yamamoto, K	1
Alagarsamy, V; Meena, R; Murugesan, S; Ramaseshu, KV; Solomon, VR; Thirumurugan, K	1
Alagarsamy, V; Raja Solomon, V; Vijayakumar, S	1
Barzaghi, M; Destro, R; Soave, R	1
Alagarsamy, V; Anjana, GV; Deepa, G; Parthiban, P; Solomon, VR	1
Al-Blowy, HA; Al-Hazimi, HM; El-Baih, FE	1
Baker, S; Brioni, JD; Chang, R; EI-Kouhen, O; Gauvin, DM; Hernandez, G; Hollingsworth, PR; Honore, P; Lehto, SG; Moreland, RB; Stewart, AO; Zheng, G; Zhu, CZ	1
Karkola, S; Lilienkampf, A; Wähälä, K	1
Butini, S; Campiani, G; Christensen, JK; Coccone, SS; De Angelis, M; Fiorini, I; Gemma, S; Guarino, E; Morelli, E; Novellino, E; Pickering, DS; Schousboe, A; Trotta, F	1
Ardayfio, P; Chen, Y; Coskun, T; Craft, L; Gehlert, DR; Li, X; Rasmussen, K; Shaw, J; Witkin, JM; Zhang, HY	1
Chen, S; Ibba, M; Patil, PB; Roy, H; Zeng, Y	1
Alho-Richmond, S; Huhtinen, K; Johansson, N; Karkola, S; Koskimies, P; Lilienkampf, A; Vihko, K; Wähälä, K	1
Bouska, JJ; Giranda, VS; Guan, R; Han, EK; Hasvold, LA; Johnson, EF; Leverson, JD; Lin, NH; Luo, Y; Penning, TD; Rosenberg, SH; Soni, N; Sowin, TJ; Stamper, G; Stewart, KD; Stoll, VS; Tao, ZF	1
Fu, L; Gu, Y; He, H; Liang, YJ; Ren, Q	1
Cho, YS; Choi, IK; Jung, HJ; Kwon, HJ	1
Fujimoto, T; Hiroe, K; Imaeda, Y; Kawamura, M; Konishi, N; Kubo, K; Shofuda, K	1
Cippitelli, A; Gehlert, DR; Heilig, M; Karlsson, C; Shaw, JL; Thorsell, A	1
Bailey, C; Barbeau, OR; Cano, C; Cockcroft, XL; Curtin, NJ; Duggan, H; Frigerio, M; Golding, BT; Griffin, RJ; Hardcastle, IR; Hummersone, MG; Knights, C; Menear, KA; Newell, DR; Richardson, CJ; Smith, GC; Spittle, B	1
Cho, YS; Kwon, HJ	1
Barbosa, J; Di Paolo, J; Liu, L; Reif, K; Rong, H; Wong, H	1
Baumgardner, M; Boggs, J; Coraggio, M; Currie, KS; Davis, JC; Deese, A; Gopaul, S; Halladay, JS; Hop, CE; Khojasteh, SC; Kuebler, P; La, H; Le, H; Liao, XC; Liu, L; Lubach, JW; Shin, Y; Sowell, CG; Wong, H; Wong, S; Young, WB	1
Buonarati, MH; Hop, CE; Jones, SA; Liu, L; Murakami, SC; Shin, YG; Wong, H	1
Aarts, M; Ashworth, A; Garcia-Murillas, I; Gevensleben, H; Hurd, MS; Sharpe, R; Shumway, SD; Toniatti, C; Turner, NC	1
Ciccocioppo, R; Cippitelli, A; Gehlert, DR; Heilig, M; Karlsson, C; Thorsell, A; Zook, M	1
Buevich, A; Caldwell, JP; Chen, X; Cox, K; Cumming, JN; Favreau, L; Greenlee, W; Grzelak, M; Hyde, L; Kazakevich, I; Kennedy, ME; Kuvelkar, R; Leach, P; Liu, X; Mandal, M; Mazzola, RD; McKittrick, BA; Orth, P; Parker, EM; Stamford, AW; Strickland, C; Terracina, G; Voigt, J; Wang, H; Zhang, L; Zhang, Q; Zhu, Z	1
Bennett, CE; Bertorelli, R; Brumfield, S; Burnett, DA; Domalski, M; Greenlee, WJ; Grilli, M; Knutson, CE; Korakas, P; Li, C; Lozza, G; Matasi, JJ; Qiang, L; Reggiani, A; Sasikumar, TK; Silverman, LS; Tulshian, D; Wu, WL	1
Mello de Queiroz, F; Pardo, LA; Stühmer, W; Valero, ML; Viana, F	1
Clapham, JC; Mitchell, S; Morgan, D; Selman, C; Sinclair, R; Speakman, JR; Zhang, LN	1
Barone, M; Cardile, V; Gemmellaro, P; Graziano, AC; Marrazzo, A; Santagati, A	1
Bishop, PW; Blackhall, F; Critchlow, SE; Dive, C; Fusi, A; Hodgkinson, CL; Kelly, P; Morrow, CJ; Nonaka, D; Polański, R; Priest, L; Smith, PD; Trapani, F; White, A	1
Babes, A; Chiritoiu, G; Cucu, D; Dima, SO; Duda, DG; Horii, A; Petrescu, S; Popescu, I; Stanica, L	1
Lubenov, LA; Mavrova, ATs; Tsenov, JA; Wesselinova, D	1
Blount, KG; Bola, BM; Chadwick, AL; Critchlow, SE; Michopoulos, F; Smith, PD; Stratford, IJ; Telfer, BA; Williams, KJ	1
Ma, HT; Mak, JP; Man, WY; Poon, RY	1
Bhatiya, A; Eguale, T; Gunn, JS; Koopman, JA; Kwiek, JJ; Marshall, JM	1
Jeong, JH; Kang, MA; Kim, JY; Kim, MS; Shin, YJ; Song, JY	1
Chapman, KL; Dexter, DT; Di Fruscia, P; Fuchter, MJ; Harrison, IF; Jung, M; Khongkow, M; Koltsida, K; Lam, EW; Laohasinnarong, S; Liu, C; Moniot, S; Reynolds, CR; Schmidtkunz, K; Steegborn, C; Sternberg, MJ; Zacharioudakis, E	1
Aktan, G; Allred, AJ; Becerra, CR; Cornfeld, M; Ferron-Brady, G; Gauvin, J; Ibrahim, N; Motwani, M; Orford, K; Papadopoulos, KP; Patnaik, A; Rasco, DW; Tolcher, AW	1
Amr, FI; Oyarzabal, J; Rabal, O	1
Blazquez-Llorca, L; Brandt Elvang, A; Filser, S; Herms, J; Jung, CK; Masana, M; Müller, MB; Ovsepian, SV; Volbracht, C	1
Barbosa, J; Blomgren, P; Bremer, MC; Crawford, JJ; Currie, KS; Dambach, D; Di Paolo, J; Gallion, S; Hymowitz, SG; Kropf, JE; Lee, SH; Liu, L; Lubach, JW; Macaluso, J; Maciejewski, P; Maurer, B; Mitchell, SA; Ortwine, DF; Reif, K; Scheerens, H; Schmitt, A; Sowell, CG; Wang, X; Wong, H; Xiong, JM; Xu, J; Young, WB; Zhao, Z	1
Das, R; Mély, Y; Sharma, R; Shin, D; Sholokh, M; Tor, Y; Zaporozhets, OA	1
Chiang, C; Cooper, MK; Fleming, JT; Frist, AY; Hao, J; Hempel, JE; Hong, CC; Sulikowski, GA; Williams, CH; Williams, MM	1
Barr, JT; Halladay, JS; Hop, CE; Jones, JP; Khojasteh, SC; Kirkpatrick, DS; Liu, L; Sodhi, JK; Wong, S	1
Cummings, J; Dive, C; Kershaw, S; Morris, K; Tugwood, J	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
Bertoni, F; Carrassa, L; Chilà, R; Damia, G; Kwee, I; Lupi, M; Restelli, V; Rinaldi, A	1
Carlsson, J; Hill, SJ; Ranganathan, A; Stoddart, LA	1
Barbosa, J; Blomgren, P; Bremer, MC; Crawford, JJ; Currie, KS; Dambach, D; Di Paolo, J; Eigenbrot, C; Gallion, S; Johnson, AR; Kropf, JE; Lee, SH; Liu, L; Lubach, JW; Macaluso, J; Maciejewski, P; Mitchell, SA; Ortwine, DF; Reif, K; Scheerens, H; Schmitt, A; Wang, X; Wong, H; Xiong, JM; Xu, J; Young, WB; Yu, C; Zhao, Z	1
Alavi, M; Bagryanova, L; Behbahan, IS; Braas, D; Chia, D; Christofk, HR; Critchlow, SE; Dubinett, SM; Espindola Camacho, C; Gardner, BK; Goodglick, L; Graeber, TG; Graham, NA; Gu, W; Hong, CS; Horvath, S; Hurvitz, SA; Krotee, PAL; Kurdistani, SK; Mah, V; Maresh, EL; Mellinghoff, IK	1
Hekmatimoghaddam, S; Pourrajab, F; Zare-Khormizi, MR	1
Ellis, CR; Hou, X; Shen, J; Tsai, CC	1
Bhat, S; Greenwood, J; Harriman, G; Harwood, HJ; Huang, X; Kapeller, R; Paul, D; Saha, AK; Tong, L; Wang, R; Westlin, WF	1
Baillie, TA; Cyrus Khojasteh, S; Dalvie, D; Rietjens, IM	1
El-Gazzar, AR; Hafez, HN; Zaki, ME	1
Ide, M; Irie, M; Kamikawa, T; Kashiwagi, H; Miura, T; Morikami, K; Muraoka, T; Nakamura, M; Nishihara, M	1
Actis, ML; Ambaye, ND; Evison, BJ; Fujii, N; Hara, K; Hashimoto, H; Heath, R; Inoue, A; Kikuchi, S; McDonald, ET; Shao, Y; Vanarotti, M	1
Aziz, AM; Barbier, E; Barchiesi, R; Gehlert, D; Heilig, M; Karlsson, C; Pitcairn, C; Rehman, F; Steensland, P; Thorsell, A; Wendel Hansen, M	1
Alachkar, A; Alhassen, L; Civelli, O; Onouye, K; Sanathara, N; Wang, L; Wang, Z	1
Bhat, S; Brun, SN; Eichner, LJ; Gerken, L; Greenwood, J; Harriman, G; Harwood, HJ; Hutchins, A; Kapeller, R; Kolar, MJ; Lombardo, PS; Metallo, CM; Parker, SJ; Saghatelian, A; Shaw, RJ; Svensson, RU; Van Nostrand, JL; Vera, L; Wallace, M; Westlin, WF	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
Kaieda, A; Kanzaki, N; Kori, M; Kuno, H; Mototani, H; Naito, T; Nara, H; Oki, H; Santou, T; Sato, K; Terauchi, J; Uchikawa, O; Yamamoto, Y	1
Beyrem, H; Chaloin, L; Clair, P; Desrumaux, C; Ghysen, A; Nasri, A; Perrier, V; Roche, DB; Valverde, AJ	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
Shaw, RJ; Svensson, RU	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
Liu, Y; Shi, M; Wang, C; Wen, Z; Xie, J; Xue, Y; Zhang, S; Zhao, L; Zhao, Y	1
Bacon, CM; Bell, N; Blair, H; Bomken, S; Critchlow, SE; Crossland, R; Keun, HC; Long, A; Miwa, S; Nakjang, S; Noble, RA; Phillips, N; Rand, V; Sikka, A; Televantou, D; Thomas, H; Wedge, SR	1
Cho, N; Hara, H; Homma, M; Iwai, K; Kurasawa, O; Miyazaki, T; Mori, K; Oguro, Y; Ohashi, A; Uchiyama, N; Yoshida, S	1
Chen, L; Ding, N; Hu, Y; Kan, C; Kan, L; Kessler, JA; Li, Y; Lu, H; McGuire, TL	1
Alachkar, A; Civelli, O; Garau, C; Nishimori, K; Sanathara, NM; Wang, L; Wang, Z; Xu, X	1
Arunan, V; Beloueche-Babari, M; Casals Galobart, T; Chung, YL; Eykyn, TR; Koniordou, M; Leach, MO; Parkes, HG; Smith, PD; Wantuch, S	1
Casey, MC; Huber, AD; Kankanala, J; Kirby, KA; Sarafianos, SG; Wang, Z; Wilson, DJ	1
Haystead, TAJ	1
Chow, MSS; Hao, J; Ramirez, A; Wang, Z; Xie, C	1
Guan, X; Morris, ME; Ruszaj, D	1
Aleem, E; Arceci, RJ; Azorsa, DO; Bista, R; Henry, MM; Lee, DW; Patel, AR; Wai, DH	1
Eichner, R; Girardi, E; Hashimoto, M; Superti-Furga, G	1
Carroll, KR; Elfers, EE; Hildeman, DA; Jordan, MB; Katz, JD; McNally, JP; Stevens, JJ	1
Boyers, A; Chadwick, A; Critchlow, SE; Mehibel, M; Mueller-Klieser, W; Ortiz-Martinez, F; Stratford, IJ; Telfer, BA; Voelxen, N; West, CM; Williams, KJ	1
Behrends, V; Bravo-Santano, N; Giskeødegård, GF; Keun, HC; Letek, M	1
Guan, X; Morris, ME; Rodriguez-Cruz, V	1
Afonso, J; Baltazar, F; Longatto-Filho, A; Marques, H; Pinheiro, C; Pinto, T; Schmitt, F; Simões-Sousa, S	1
Dutta, S; Nandi, N; Saha, A	1
Chen, CP; Feng, ZQ; Li, EQ; Liu, SJ; Qin, LZ; Wen, X; Zhang, C; Zhao, W	1
Abdelrahman, MH; Aboraia, AS; Abuo-Rahma, GEA; Elsadek, BEM; Mohamed, MFA; Shaykoon, MSA; Youssif, BGM	1
Chang, S; Choi, EA; Choi, YS; Kim, SC; Lee, EJ; Singh, SR	1
Bailey, TL; McDonald, PH; Nieto, A	1
Guan, X; Morris, ME	2
Chen, Z; Fan, PH; Liu, HW; Ushimaru, R; Zhao, H	1
Cho, N; Hara, H; Hoffman, I; Homma, M; Imada, T; Iwai, K; Iwata, K; Kurasawa, O; Miyazaki, T; Nomura, T; Oguro, Y; Ohashi, A; Ohori, M; Skene, R; Sugimoto, H; Uchiyama, N; Yamamoto, Y	1
Beloueche-Babari, M; Casals Galobart, T; Delgado-Goni, T; Harker, JA; Leach, MO; Parkes, HG; Tandy, D; Wantuch, S	1
Anant, S; Andronache, I; Biersack, B; Dandawate, P; Gold, M; Köhler, L; Lanzloth, C; Schobert, R	1
Bacon, C; Bowron, A; Greystoke, A; Halford, S; Jenkinson, F; Keun, H; Leech, N; McNeillis, R; Petrides, G; Plummer, R; Siskos, A; Walton, J	1
Balsamo, JA; Giorgio, TD; Glass, EB; Haycook, CP; Hong, CC; Major, AS; Williams, CH	1
Juvale, K; Puri, S	1
Barakat, A; Boraei, ATA; Eltamany, EH; Gad, EM; Hammad, MSAG; Nafie, MS	1
Allen, AE; Grant, C; Greenwood, K; Lucas, RJ; Martin, EA; Redfern, WS; Vince, P	1
Beutler, JA; Caboni, P; Corona, A; Esposito, F; Laus, A; Le Grice, SFJ; Tocco, G; Tramontano, E; Wilson, JA	1
Jiang, X; Lei, J; Wang, N; Xu, H; Yan, C; Yuan, Y; Zhang, S; Zhu, A	1
Benes, CH; Boikos, SA; Calbert, ML; Dalton, KM; Dozmorov, M; Egan, RK; Faber, AC; Floros, KV; Glod, J; Greninger, P; Hu, B; Koblinski, J; Kurupi, R; Lochmann, TL; McClanaghan, J; Murchie, E; Puchalapalli, M; Ramamoorthy, S; Shock, L; Stein, GT	1
Eliopoulos, E; Papakonstantinou, E; Thireou, T; Vlachakis, D; Vlachoyiannopoulos, PG	1
Ademi, H; Chaachouay, H; Gassmann, M; Gerst, D; Gorr, TA; Shinde, DA; Vogel, J	1
Li, J; Li, W; Na, N; Ouyang, J; Zhang, S; Zhang, Y	1
Alachkar, A; Alhassen, W; Kobayashi, Y; Myint, T; Nauli, SM; Nguyen, H; Robbins, B; Saito, Y; Su, J; Yu, M	1
Bergthaler, A; Bigenzahn, JW; César-Razquin, A; Kartnig, F; Kornauth, C; Lercher, A; Pemovska, T; Srndic, I; Staber, PB; Superti-Furga, G; Valent, P	1
Ioannidis, M; Janssens, MH; Mesman, RJ; Revelo, NH; Stempels, FC; Ter Beest, M; van den Bogaart, G	1
Afonso, J; Antunes, B; Baltazar, F; Batista, A; Pinto-Ribeiro, F; Silva, A	1
Bailey, T; McDonald, P; Nieto, A	1
Bacon, CM; Banerji, U; Chénard-Poirier, M; Dragoni, I; Greystoke, A; Halford, S; Heinzmann, K; Howell, EC; Innes, WA; Keun, HC; Morris, K; Payne, GS; Petrides, G; Plummer, C; Plummer, R; Potter, S; Rata, M; Salisbury, BM; Sloan, P; Veal, GJ; Wedge, SR	1

Reviews

6 review(s) available for thiophenes and pyrimidinones

Article	Year
Control of autophagy with small molecules. Archives of pharmacal research, 2010, Volume: 33, Issue:12 Topics: Alzheimer Disease; Autophagy; Cell Death; Humans; Neurodegenerative Diseases; Parkinson Disease; Proteins; Pyrimidinones; Signal Transduction; Small Molecule Libraries; Structure-Activity Relationship; Thiophenes	2010
Underlying mechanisms and chemical/biochemical therapeutic approaches to ameliorate protein misfolding neurodegenerative diseases. BioFactors (Oxford, England), 2017, Volume: 43, Issue:6 Topics: Amyloidogenic Proteins; Animals; Chalcones; Endoplasmic Reticulum; Gene Expression Regulation; Heat-Shock Response; Humans; Hydrazones; Molecular Chaperones; Neurodegenerative Diseases; Neuroprotective Agents; Protein Aggregation, Pathological; Protein Folding; Proteostasis; Proteostasis Deficiencies; Pyrimidinones; Thiophenes; Unfolded Protein Response	2017
Biotransformation and bioactivation reactions - 2015 literature highlights. Drug metabolism reviews, 2016, Volume: 48, Issue:2 Topics: Acetaminophen; Allylbenzene Derivatives; Aniline Compounds; Animals; Anisoles; Benzbromarone; Biotransformation; Humans; Imidazoles; Niacinamide; Nitroimidazoles; Nitrosamines; Oxazoles; Oxazolidinones; Peroxides; Pyrazines; Pyrazoles; Pyridazines; Pyridines; Pyridones; Pyrimidinones; Thiophenes; Triazoles	2016
Lipid Synthesis Is a Metabolic Liability of Non-Small Cell Lung Cancer. Cold Spring Harbor symposia on quantitative biology, 2016, Volume: 81 Topics: Acetyl-CoA Carboxylase; Animals; Carcinoma, Non-Small-Cell Lung; Fatty Acids; Gene Regulatory Networks; Humans; Models, Animal; Pyrimidinones; Thiophenes	2016
Monocarboxylate transporter 1 and 4 inhibitors as potential therapeutics for treating solid tumours: A review with structure-activity relationship insights. European journal of medicinal chemistry, 2020, Aug-01, Volume: 199 Topics: Antineoplastic Agents; Drug Resistance, Neoplasm; Humans; Monocarboxylic Acid Transporters; Muscle Proteins; Neoplasms; Pyrimidinones; Structure-Activity Relationship; Symporters; Thiophenes; Uracil	2020
In Vivo Anticancer Activity of AZD3965: A Systematic Review. Molecules (Basel, Switzerland), 2021, Dec-29, Volume: 27, Issue:1 Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Disease Management; Disease Progression; Drug Evaluation, Preclinical; Energy Metabolism; Glycolysis; Humans; Lactic Acid; Monocarboxylic Acid Transporters; Neoplasms; Pyrimidinones; Signal Transduction; Symporters; Thiophenes; Tumor Microenvironment; Warburg Effect, Oncologic; Xenograft Model Antitumor Assays	2021

Trials

4 trial(s) available for thiophenes and pyrimidinones

Article	Year
Clinical and hormonal effects of the new angiotensin II receptor antagonist LRB081. Journal of cardiovascular pharmacology, 1996, Volume: 28, Issue:2 Topics: Adult; Aldosterone; Angiotensin II; Angiotensin Receptor Antagonists; Blood Pressure; Catecholamines; Double-Blind Method; Hormones; Humans; Male; Pyrimidinones; Regional Blood Flow; Renin; Thiophenes	1996
Validation and application of a liquid chromatography-tandem mass spectrometric method for the determination of GDC-0834 and its metabolite in human plasma using semi-automated 96-well protein precipitation. Biomedical chromatography : BMC, 2012, Volume: 26, Issue:11 Topics: Chemical Precipitation; Chromatography, Liquid; Double-Blind Method; Drug Stability; Humans; Linear Models; Pyrimidinones; Reproducibility of Results; Sensitivity and Specificity; Tandem Mass Spectrometry; Thiophenes	2012
Phase I study of the MEK inhibitor trametinib in combination with the AKT inhibitor afuresertib in patients with solid tumors and multiple myeloma. Cancer chemotherapy and pharmacology, 2015, Volume: 75, Issue:1 Topics: Adult; Aged; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Cohort Studies; Dose-Response Relationship, Drug; Early Termination of Clinical Trials; Female; Humans; Male; MAP Kinase Kinase 1; MAP Kinase Kinase 2; Middle Aged; Multiple Myeloma; Neoplasms; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-akt; Pyrazoles; Pyridones; Pyrimidinones; Thiophenes; Tumor Burden	2015
A Phase I Dose-escalation Study of AZD3965, an Oral Monocarboxylate Transporter 1 Inhibitor, in Patients with Advanced Cancer. Clinical cancer research : an official journal of the American Association for Cancer Research, 2023, 04-14, Volume: 29, Issue:8 Topics: Antineoplastic Agents; Dose-Response Relationship, Drug; Humans; Maximum Tolerated Dose; Neoplasms; Pyrimidinones; Thiophenes	2023

Other Studies

129 other study(ies) available for thiophenes and pyrimidinones

Article	Year
[New basically substituted pyrimidines and benzothienopyrimidines]. Archiv der Pharmazie, 1977, Volume: 26, Issue:4 Topics: Indicators and Reagents; Magnetic Resonance Spectroscopy; Pyrimidinones; Thiophenes	1977
Synthesis of 3-substituted thieno [2, 3-d] pyrimidin-4(3H)-one-2-mercaptoacetic acids and their ethyl esters for pharmacological screening. Journal of pharmaceutical sciences, 1976, Volume: 65, Issue:5 Topics: Analgesics; Animals; Anti-Bacterial Agents; Anti-Inflammatory Agents; Anticonvulsants; Bacteria; Chemistry, Pharmaceutical; Drug Evaluation, Preclinical; Female; Male; Mice; Pyrimidinones; Rats; Sulfhydryl Compounds; Thiophenes	1976
Synthesis and antimicrobial activity of some thiazolinyl tetrahydrobenzo[b]thiophenes and thiazolinyl tetrahydrobenzothieno[2,3-d]pyrimidin-4-ones. Farmaco (Societa chimica italiana : 1989), 1992, Volume: 47, Issue:5 Topics: Anti-Bacterial Agents; Anti-Infective Agents; Antifungal Agents; Candida albicans; Escherichia coli; Microbial Sensitivity Tests; Nystatin; Pyrimidinones; Staphylococcus aureus; Thiazoles; Thiophenes	1992
Synthesis and pharmacological activity of 2-alkylthio substituted thieno[2,3-d]pyrimidine-4-one and 5H-pyrimido [5,4-b]indol-4-one. Die Pharmazie, 1990, Volume: 45, Issue:7 Topics: Animals; Aorta, Thoracic; Charcoal; Chemical Phenomena; Chemistry; Guinea Pigs; Ileum; In Vitro Techniques; Indoles; Male; Mice; Muscle Contraction; Muscle, Smooth; Muscle, Smooth, Vascular; Parasympatholytics; Pyrimidines; Pyrimidinones; Rabbits; Thiophenes	1990
[Synthesis and analgesic activity of 3-substituted derivatives of pyrido [3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-ones]. Il Farmaco; edizione scientifica, 1985, Volume: 40, Issue:11 Topics: Analgesics; Animals; Chemical Phenomena; Chemistry; Mice; Mice, Inbred Strains; Pyridines; Pyrimidinones; Rats; Rats, Inbred Strains; Schiff Bases; Stomach Diseases; Thiophenes	1985
Heterocyclic compounds. 4. Synthesis and antiinflammatory activity of some substituted thienopyrimidones. Journal of medicinal chemistry, 1972, Volume: 15, Issue:1 Topics: Administration, Oral; Animals; Anti-Inflammatory Agents; Edema; Lethal Dose 50; Mice; Pyrimidinones; Thiophenes	1972
N-3-substituted pyrimidinones as potent, orally active, AT1 selective angiotensin II receptor antagonists. Journal of medicinal chemistry, 1995, Nov-24, Volume: 38, Issue:24 Topics: Administration, Oral; Angiotensin Receptor Antagonists; Animals; Humans; Hypertension; Male; Models, Molecular; Molecular Conformation; Molecular Structure; Pyrimidinones; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship; Thiophenes	1995
The selective angiotensin AT1 receptor antagonist LR-B/081 potently inhibits drinking induced by central injection of angiotensin II in rats. European journal of pharmacology, 1995, Apr-24, Volume: 277, Issue:2-3 Topics: Analysis of Variance; Angiotensin II; Angiotensin Receptor Antagonists; Animals; Antihypertensive Agents; Biphenyl Compounds; Carbachol; Dose-Response Relationship, Drug; Drinking; Eating; Imidazoles; Injections, Intraventricular; Lethal Dose 50; Losartan; Male; Milk; Pyrimidinones; Rats; Rats, Wistar; Renin-Angiotensin System; Tetrazoles; Thiophenes	1995
Pharmacology of LR-B/081, a new highly potent, selective and orally active, nonpeptide angiotensin II AT1 receptor antagonist. British journal of pharmacology, 1995, Volume: 114, Issue:6 Topics: Administration, Oral; Angiotensin Receptor Antagonists; Animals; Aorta; Blood Pressure; Decerebrate State; In Vitro Techniques; Male; Perfusion; Pyrimidinones; Rabbits; Rats; Rats, Inbred SHR; Rats, Sprague-Dawley; Thiophenes; Vasoconstriction	1995
Synthesis of 2,3-dihydro-3-amino-6-phenyl-2-thioxothieno [2,3-d] pyrimidin-4 (1H)-one and of potential antiinflammatory agents 2-aryl-7-phenyl-3H, 9H-pyrimido [2,1-b]thieno-[2',3':4,5]]1,3,4] thiadiazin-9-ones. Die Pharmazie, 1994, Volume: 49, Issue:1 Topics: Acetates; Acetic Acid; Animals; Anti-Inflammatory Agents, Non-Steroidal; Benzoquinones; Carrageenan; Edema; Magnetic Resonance Spectroscopy; Pain Measurement; Peritonitis; Pyrimidines; Pyrimidinones; Rats; Spectrophotometry, Infrared; Thiadiazines; Thiophenes	1994
Angiotensin II-induced responses in vascular smooth muscle cells: inhibition by non-peptide receptor antagonists. European journal of pharmacology, 1995, Jul-14, Volume: 280, Issue:3 Topics: Angiotensin II; Angiotensin Receptor Antagonists; Animals; Aorta, Thoracic; Biphenyl Compounds; Cells, Cultured; Dinoprostone; DNA; Epoprostenol; Imidazoles; Inositol 1,4,5-Trisphosphate; Leucine; Losartan; Male; Muscle, Smooth, Vascular; Protein Biosynthesis; Pyridines; Pyrimidinones; Rats; Rats, Sprague-Dawley; Tetrazoles; Thiophenes; Thymidine	1995
Molecular pharmacology of LR-B/081, a new non-peptide angiotensin AT1 receptor antagonist. European journal of pharmacology, 1995, Jul-18, Volume: 290, Issue:2 Topics: Adrenal Cortex; Angiotensin Receptor Antagonists; Animals; Binding, Competitive; Cattle; Cerebellum; Humans; Male; Molecular Structure; Pyrimidinones; Rats; Thiophenes	1995
Synthesis and pharmacological evaluation of thieno[2,3-d]pyrimidin-2,4-dione and 5H-pyrimido [5,4-b]indol-2,4-dione derivatives. Farmaco (Societa chimica italiana : 1989), 1995, Volume: 50, Issue:10 Topics: Analgesics, Non-Narcotic; Animals; Anti-Inflammatory Agents, Non-Steroidal; Bacteria; Behavior, Animal; Carrageenan; Deuterium; Fungi; Indoles; Inflammation; Magnetic Resonance Spectroscopy; Male; Mice; Microbial Sensitivity Tests; Pain Measurement; Peritonitis; Pyrimidinones; Rats; Rats, Sprague-Dawley; Stomach Ulcer; Thiophenes	1995
Functional evidence for the ability of angiotensin AT1 receptor antagonists to cross the blood-brain barrier in rats. European journal of pharmacology, 1996, Jul-04, Volume: 307, Issue:3 Topics: Administration, Oral; Angiotensin II; Angiotensin Receptor Antagonists; Animals; Antihypertensive Agents; Biphenyl Compounds; Blood Pressure; Blood-Brain Barrier; Carbachol; Dose-Response Relationship, Drug; Drinking; Imidazoles; Injections, Intraperitoneal; Injections, Intraventricular; Losartan; Male; Nicotinic Acids; Pyrimidinones; Rats; Rats, Wistar; Receptor, Angiotensin, Type 1; Tetrazoles; Thiophenes	1996
Synthesis and evaluation of 2-chloromethyl-3-N-substituted arylthieno (2,3-d)pyrimidin-4-ones and derivatives for central nervous system depressant activity. Arzneimittel-Forschung, 1997, Volume: 47, Issue:9 Topics: Animals; Central Nervous System Depressants; Chemical Phenomena; Chemistry, Physical; Mass Spectrometry; Mice; Postural Balance; Pyrimidinones; Spectrophotometry, Infrared; Spectrophotometry, Ultraviolet; Thiophenes	1997
New azole antifungals. 2. Synthesis and antifungal activity of heterocyclecarboxamide derivatives of 3-amino-2-aryl-1-azolyl-2-butanol. Journal of medicinal chemistry, 1998, May-21, Volume: 41, Issue:11 Topics: Animals; Antifungal Agents; Aspergillosis; Aspergillus fumigatus; Candidiasis; Colony Count, Microbial; Fungi; Male; Mice; Molecular Conformation; Pyrimidinones; Rats; Stereoisomerism; Structure-Activity Relationship; Thiazoles; Thiophenes; Triazoles	1998
Synthesis of thiophenecarboxamides, thieno[3,4-c]pyridin-4(5H)-ones and thieno[3,4-d]pyrimidin-4(3H)-ones and preliminary evaluation as inhibitors of poly(ADP-ribose)polymerase (PARP). Bioorganic & medicinal chemistry, 1999, Volume: 7, Issue:2 Topics: Animals; Cell Line; Inhibitory Concentration 50; Magnetic Resonance Spectroscopy; Mice; Models, Chemical; Poly(ADP-ribose) Polymerase Inhibitors; Pyridones; Pyrimidinones; Thiophenes	1999
High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor. Bioorganic & medicinal chemistry letters, 2000, May-15, Volume: 10, Issue:10 Topics: Animals; Binding Sites; Ligands; Piperazine; Piperazines; Pyrimidinones; Rats; Receptors, Adrenergic, alpha-1; Receptors, Serotonin; Receptors, Serotonin, 5-HT1; Serotonin; Structure-Activity Relationship; Thiophenes	2000
Synthesis and antitumor activity of thieno-separated tricyclic purines. Journal of medicinal chemistry, 2000, Dec-14, Volume: 43, Issue:25 Topics: Antineoplastic Agents; Cell Division; Colorectal Neoplasms; Drug Screening Assays, Antitumor; Humans; Purines; Pyrimidines; Pyrimidinones; Thiophenes; Tumor Cells, Cultured	2000
A potent seryl tRNA synthetase inhibitor SB-217452 isolated from a Streptomyces species. The Journal of antibiotics, 2000, Volume: 53, Issue:12 Topics: Animals; Enzyme Inhibitors; Magnetic Resonance Spectroscopy; Molecular Structure; Pyrimidinones; Rats; Serine-tRNA Ligase; Spectrometry, Mass, Fast Atom Bombardment; Staphylococcus aureus; Streptomyces; Thiophenes	2000
Synthesis and spasmolytic action of 2-substituted thienopyrimidin-4-one derivatives. The Journal of pharmacy and pharmacology, 2002, Volume: 54, Issue:5 Topics: Animals; Calcium Channels, L-Type; Electric Stimulation; Guinea Pigs; Ileum; In Vitro Techniques; Male; Mice; Muscle Contraction; Muscle, Smooth; Parasympatholytics; Pyrimidinones; Rats; Rats, Sprague-Dawley; Receptors, Muscarinic; Thiophenes	2002
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists. Bioorganic & medicinal chemistry letters, 2003, Oct-20, Volume: 13, Issue:20 Topics: Pyrimidinones; Receptors, LHRH; Structure-Activity Relationship; Thiophenes	2003
Progress in the understanding of drug-receptor interactions, Part 1: experimental charge-density study of an angiotensin II receptor antagonist (C30H30N6O3S) at T = 17 K. Chemistry (Weinheim an der Bergstrasse, Germany), 2005, Aug-05, Volume: 11, Issue:16 Topics: Angiotensin Receptor Antagonists; Antihypertensive Agents; Cold Temperature; Humans; Molecular Conformation; Molecular Structure; Pyrimidinones; Static Electricity; Thiophenes; X-Ray Diffraction	2005
Induction of apoptosis by photoexcited tetracyclic compounds derivatives of benzo[b]thiophenes and pyridines. Journal of photochemistry and photobiology. B, Biology, 2006, Feb-01, Volume: 82, Issue:2 Topics: Apoptosis; Cell Cycle; Cell Line, Tumor; Drug Screening Assays, Antitumor; Heterocyclic Compounds, 4 or More Rings; HL-60 Cells; Humans; Jurkat Cells; Photosensitizing Agents; Pyridines; Pyrimidinones; Thiophenes	2006
Exploration of a new type of antimalarial compounds based on febrifugine. Journal of medicinal chemistry, 2006, Jul-27, Volume: 49, Issue:15 Topics: Animals; Antimalarials; Cell Line; Malaria; Mice; Parasitic Sensitivity Tests; Piperidines; Plasmodium berghei; Plasmodium falciparum; Pyrimidinones; Quinazolines; Stereoisomerism; Structure-Activity Relationship; Thiophenes; Toxicity Tests, Acute	2006
Design and synthesis of 2-methylthio-3-substituted-5,6-dimethylthieno [2,3-d] pyrimidin-4(3H)-ones as analgesic, anti-inflammatory and antibacterial agents. Medicinal chemistry (Shariqah (United Arab Emirates)), 2007, Volume: 3, Issue:1 Topics: Analgesics, Non-Narcotic; Animals; Anti-Bacterial Agents; Anti-Inflammatory Agents, Non-Steroidal; Bacteria; Carrageenan; Drug Design; Edema; Indicators and Reagents; Magnetic Resonance Spectroscopy; Microbial Sensitivity Tests; Pain Measurement; Pyrimidinones; Rats; Reaction Time; Structure-Activity Relationship; Thiophenes; Thiourea	2007
Synthesis of 2-mercapto-3-substituted-5,6-dimethylthieno[2,3-d] pyrimidin-4(3H)-ones as new analgesic, anti-inflammatory agents. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, 2007, Volume: 61, Issue:5 Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Dose-Response Relationship, Drug; Pain Measurement; Pyrimidinones; Rats; Rats, Wistar; Stomach Ulcer; Structure-Activity Relationship; Sulfhydryl Compounds; Thiophenes	2007
Progress in the understanding of drug-receptor interactions, part 2: experimental and theoretical electrostatic moments and interaction energies of an angiotensin II receptor antagonist (C30H30N6(O)3S). Chemistry (Weinheim an der Bergstrasse, Germany), 2007, Volume: 13, Issue:24 Topics: Angiotensin Receptor Antagonists; Gases; Hydrogen Bonding; Models, Molecular; Molecular Structure; Pyrimidinones; Receptors, Angiotensin; Static Electricity; Thiophenes; X-Ray Diffraction	2007
Synthesis and pharmacological investigation of 3-subsituted-amino-2-methylsulfanyl-5,6,7,8-tetrahydro-3H-benzo[4,5]thieno[2,3-d]pyrimidin-4-ones as analgesic and anti-inflammatory agents. Archiv der Pharmazie, 2007, Volume: 340, Issue:7 Topics: Analgesics; Animals; Anti-Inflammatory Agents, Non-Steroidal; Edema; Female; Magnetic Resonance Spectroscopy; Male; Pain Measurement; Pyrimidinones; Rats; Rats, Wistar; Stomach Ulcer; Structure-Activity Relationship; Sulfones; Thiophenes	2007
Synthesis of some thienopyrimidine derivatives. Molecules (Basel, Switzerland), 2006, Jul-05, Volume: 11, Issue:7 Topics: Pyrimidines; Pyrimidinones; Thiophenes	2006
Analgesic activity of metabotropic glutamate receptor 1 antagonists on spontaneous post-operative pain in rats. European journal of pharmacology, 2008, Feb-12, Volume: 580, Issue:3 Topics: Analgesics, Non-Narcotic; Animals; Calcium; Cell Membrane; Cerebellum; Dimethylamines; Dose-Response Relationship, Drug; Excitatory Amino Acid Antagonists; Exploratory Behavior; Fluorometry; Glycine; Heterocyclic Compounds, 3-Ring; Hindlimb; Male; Molecular Structure; Morphine; Pain, Postoperative; Pyridines; Pyrimidinones; Radioligand Assay; Rats; Rats, Sprague-Dawley; Receptors, Metabotropic Glutamate; Resorcinols; Rotarod Performance Test; Thiophenes; Tritium	2008
A 3D QSAR model of 17beta-HSD1 inhibitors based on a thieno[2,3-d]pyrimidin-4(3H)-one core applying molecular dynamics simulations and ligand-protein docking. ChemMedChem, 2008, Volume: 3, Issue:3 Topics: 17-Hydroxysteroid Dehydrogenases; Algorithms; Binding Sites; Breast Neoplasms; Catalysis; Computer Simulation; Enzyme Inhibitors; Female; Humans; Ligands; Molecular Conformation; NADP; Pyrimidinones; Quantitative Structure-Activity Relationship; Thiophenes	2008
1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators. Journal of medicinal chemistry, 2008, Oct-23, Volume: 51, Issue:20 Topics: Animals; Cell Line; Electrophysiology; Excitatory Amino Acid Antagonists; Female; Humans; Ligands; Molecular Structure; Oocytes; Pyrimidinones; Rats; Receptors, Glutamate; Spodoptera; Structure-Activity Relationship; Thiophenes; Xenopus laevis	2008
Preclinical evaluation of melanin-concentrating hormone receptor 1 antagonism for the treatment of obesity and depression. The Journal of pharmacology and experimental therapeutics, 2009, Volume: 329, Issue:2 Topics: Animals; Anti-Obesity Agents; Antidepressive Agents; Autoradiography; Behavior, Animal; Body Weight; Depression; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Male; Mice; Mice, Knockout; Motor Activity; Obesity; Protein Binding; Pyrimidinones; Rats; Rats, Long-Evans; Rats, Sprague-Dawley; Receptors, Somatostatin; Social Dominance; Swimming; Thiophenes	2009
Characterization of two seryl-tRNA synthetases in albomycin-producing Streptomyces sp. strain ATCC 700974. Antimicrobial agents and chemotherapy, 2009, Volume: 53, Issue:11 Topics: Amino Acid Sequence; Anti-Bacterial Agents; Ferrichrome; Molecular Sequence Data; Multigene Family; Pyrimidinones; Serine; Serine-tRNA Ligase; Streptomyces; Thiophenes	2009
Synthesis and biological evaluation of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitors based on a thieno[2,3-d]pyrimidin-4(3H)-one core. Journal of medicinal chemistry, 2009, Nov-12, Volume: 52, Issue:21 Topics: 17-Hydroxysteroid Dehydrogenases; Antineoplastic Agents; Azepines; Breast Neoplasms; Cell Line, Tumor; Estradiol Dehydrogenases; Estrogen Receptor alpha; Estrogen Receptor beta; Estrogens; Female; Humans; Isoenzymes; Models, Molecular; Neoplasms, Hormone-Dependent; Pyrimidinones; Recombinant Proteins; Structure-Activity Relationship; Thiophenes	2009
Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases. Journal of medicinal chemistry, 2009, Nov-12, Volume: 52, Issue:21 Topics: Administration, Oral; Animals; Antineoplastic Agents; bcl-Associated Death Protein; Biological Availability; Cell Line, Tumor; Cell Membrane Permeability; Humans; In Vitro Techniques; Mice; Microsomes, Liver; Models, Molecular; Phosphorylation; Protein Conformation; Proto-Oncogene Proteins c-pim-1; Pyrimidines; Pyrimidinones; Structure-Activity Relationship; Thiophenes	2009
A facile synthesis and biological activity of novel tetrahydrobenzo[4',5']thieno[3',2':5,6]pyrido[4,3-d]pyrimidin-4(3H)-ones. Bioorganic & medicinal chemistry letters, 2009, Dec-01, Volume: 19, Issue:23 Topics: Antifungal Agents; Antineoplastic Agents; Botrytis; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Humans; KB Cells; Microbial Sensitivity Tests; Molecular Structure; Pyrimidinones; Structure-Activity Relationship; Thiophenes	2009
Autophagonizer, a novel synthetic small molecule, induces autophagic cell death. Biochemical and biophysical research communications, 2010, Mar-19, Volume: 393, Issue:4 Topics: Antineoplastic Agents; Apoptosis; Autophagy; Cell Line, Tumor; Cell Proliferation; Cell Survival; Humans; Pyrimidinones; Thiophenes	2010
Antithrombotic and anticoagulant profiles of TAK-442, a novel factor Xa inhibitor, in a rabbit model of venous thrombosis. Journal of cardiovascular pharmacology, 2010, Volume: 56, Issue:2 Topics: Animals; Anticoagulants; Azetidines; Benzylamines; Bleeding Time; Blood Coagulation; Blood Coagulation Tests; Dogs; Factor Xa Inhibitors; Fibrinolytic Agents; Humans; Macaca fascicularis; Male; Mice; Mice, Inbred ICR; Morpholines; Pyrazoles; Pyridones; Pyrimidinones; Rabbits; Rats; Rats, Sprague-Dawley; Rivaroxaban; Sulfones; Thiophenes; Thrombin; Venous Thrombosis	2010
Suppression of alcohol self-administration and reinstatement of alcohol seeking by melanin-concentrating hormone receptor 1 (MCH1-R) antagonism in Wistar rats. Psychopharmacology, 2010, Volume: 211, Issue:4 Topics: Alcohol Drinking; Animals; Anti-Obesity Agents; Dose-Response Relationship, Drug; Drug Delivery Systems; Male; Motor Activity; Pyrimidinones; Rats; Rats, Wistar; Receptors, Somatostatin; Reward; Secondary Prevention; Self Administration; Taste; Thiophenes	2010
DNA-dependent protein kinase (DNA-PK) inhibitors. Synthesis and biological activity of quinolin-4-one and pyridopyrimidin-4-one surrogates for the chromen-4-one chemotype. Journal of medicinal chemistry, 2010, Dec-23, Volume: 53, Issue:24 Topics: Benzopyrans; Cell Membrane Permeability; DNA Damage; DNA-Activated Protein Kinase; Furans; HeLa Cells; Humans; Pyridines; Pyrimidinones; Quinolones; Small Molecule Libraries; Structure-Activity Relationship; Thiophenes	2010
Antiarthritis effect of a novel Bruton's tyrosine kinase (BTK) inhibitor in rat collagen-induced arthritis and mechanism-based pharmacokinetic/pharmacodynamic modeling: relationships between inhibition of BTK phosphorylation and efficacy. The Journal of pharmacology and experimental therapeutics, 2011, Volume: 338, Issue:1 Topics: Agammaglobulinaemia Tyrosine Kinase; Animals; Antirheumatic Agents; Arthritis, Experimental; Cattle; Female; Male; Mice; Mice, Inbred BALB C; Models, Chemical; Phosphorylation; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrimidinones; Rats; Rats, Inbred Lew; Rats, Sprague-Dawley; Thiophenes; Treatment Outcome	2011
Significant species difference in amide hydrolysis of GDC-0834, a novel potent and selective Bruton's tyrosine kinase inhibitor. Drug metabolism and disposition: the biological fate of chemicals, 2011, Volume: 39, Issue:10 Topics: Agammaglobulinaemia Tyrosine Kinase; Amides; Animals; Cells, Cultured; Clinical Trials, Phase I as Topic; Dogs; Double-Blind Method; Female; Hepatocytes; Humans; Hydrolysis; Macaca fascicularis; Male; Mice; Microsomes, Liver; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrimidinones; Randomized Controlled Trials as Topic; Rats; Rats, Sprague-Dawley; Species Specificity; Thiophenes	2011
Forced mitotic entry of S-phase cells as a therapeutic strategy induced by inhibition of WEE1. Cancer discovery, 2012, Volume: 2, Issue:6 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
Melanin-concentrating hormone receptor 1 (MCH1-R) antagonism: reduced appetite for calories and suppression of addictive-like behaviors. Pharmacology, biochemistry, and behavior, 2012, Volume: 102, Issue:3 Topics: Animals; Appetite; Behavior, Addictive; Carbohydrates; Conditioning, Operant; Cues; Energy Intake; Environment; Male; Motivation; Pyrimidinones; Rats; Rats, Wistar; Receptors, Somatostatin; Recurrence; Reinforcement Schedule; Saccharin; Self Administration; Thiophenes	2012
Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation. Journal of medicinal chemistry, 2012, Nov-08, Volume: 55, Issue:21 Topics: Administration, Oral; Amyloid beta-Peptides; Amyloid Precursor Protein Secretases; Animals; Aspartic Acid Endopeptidases; Bridged Bicyclo Compounds, Heterocyclic; Cerebral Cortex; Crystallography, X-Ray; HEK293 Cells; Humans; Macaca fascicularis; Models, Molecular; Molecular Conformation; Nitriles; Peptide Fragments; Permeability; Pyrimidines; Pyrimidinones; Quantum Theory; Rats; Stereoisomerism; Structure-Activity Relationship; Thermodynamics; Thiophenes	2012
Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain. Bioorganic & medicinal chemistry letters, 2012, Dec-01, Volume: 22, Issue:23 Topics: Administration, Oral; Animals; Chronic Pain; Disease Models, Animal; Heterocyclic Compounds, 3-Ring; Humans; Pyrimidinones; Rats; Receptors, Metabotropic Glutamate; Structure-Activity Relationship; Thiophenes	2012
TRPM8 ion channels differentially modulate proliferation and cell cycle distribution of normal and cancer prostate cells. PloS one, 2012, Volume: 7, Issue:12 Topics: Benzamides; Cell Cycle; Cell Line; Cell Line, Tumor; Cell Proliferation; Humans; Ion Channels; Male; Menthol; Prostate; Prostatic Neoplasms; Pyrimidinones; Thiophenes; Transfection; TRPM Cation Channels; Wound Healing	2012
Effects of a specific MCHR1 antagonist (GW803430) on energy budget and glucose metabolism in diet-induced obese mice. Obesity (Silver Spring, Md.), 2014, Volume: 22, Issue:3 Topics: Absorptiometry, Photon; Adipose Tissue; Administration, Oral; Animals; Body Mass Index; Diet, High-Fat; Energy Intake; Energy Metabolism; Glucose; Glucose Tolerance Test; Homeostasis; Insulin; Leptin; Male; Mice; Mice, Inbred C57BL; Mice, Obese; Motor Activity; Obesity; Pyrimidinones; Receptors, Somatostatin; Thiophenes; Triglycerides; Weight Loss	2014
Synthesis and biological evaluation of new benzo-thieno[3,2-d]pyrimidin-4-one sulphonamide thio-derivatives as potential selective cyclooxygenase-2 inhibitors. Molecular diversity, 2013, Volume: 17, Issue:3 Topics: Animals; Anti-Inflammatory Agents; Cell Line; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Heterocyclic Compounds, 3-Ring; Humans; Intercellular Adhesion Molecule-1; Interferon-gamma; Interleukin-8; Keratinocytes; Lipopolysaccharides; Macrophages; Mice; Monocytes; Nitric Oxide Synthase Type II; Prostaglandins E; Pyrimidinones; Thiophenes	2013
Activity of the monocarboxylate transporter 1 inhibitor AZD3965 in small cell lung cancer. Clinical cancer research : an official journal of the American Association for Cancer Research, 2014, Feb-15, Volume: 20, Issue:4 Topics: Adult; Aged; Aged, 80 and over; Animals; Antineoplastic Agents; Cell Death; Cell Line, Tumor; Drug Resistance, Neoplasm; Female; Humans; Inhibitory Concentration 50; Kaplan-Meier Estimate; Lactic Acid; Lung Neoplasms; Male; Mice; Mice, Inbred NOD; Mice, SCID; Middle Aged; Monocarboxylic Acid Transporters; Multivariate Analysis; Muscle Proteins; Pyrimidinones; Small Cell Lung Carcinoma; Symporters; Thiophenes; Xenograft Model Antitumor Assays	2014
Characterization of functional transient receptor potential melastatin 8 channels in human pancreatic ductal adenocarcinoma cells. Pancreas, 2014, Volume: 43, Issue:5 Topics: Adenocarcinoma; Benzamides; Blotting, Western; Carcinoma, Pancreatic Ductal; Cell Line; Cell Line, Tumor; Cell Membrane; Cell Movement; HEK293 Cells; Humans; Immunohistochemistry; Membrane Potentials; Membrane Proteins; Menthol; Pancreatic Neoplasms; Patch-Clamp Techniques; Pyrimidinones; RNA Interference; Thiophenes; TRPM Cation Channels	2014
Synthesis and antiproliferative activity of some new thieno[2,3-d]pyrimidin-4(3H)-ones containing 1,2,4-triazole and 1,3,4-thiadiazole moiety. European journal of medicinal chemistry, 2014, Oct-30, Volume: 86 Topics: Antineoplastic Agents; Cell Line; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; HeLa Cells; Hep G2 Cells; HT29 Cells; Humans; Molecular Structure; Pyrimidinones; Structure-Activity Relationship; Thiadiazoles; Thiophenes; Triazoles	2014
Inhibition of monocarboxylate transporter-1 (MCT1) by AZD3965 enhances radiosensitivity by reducing lactate transport. Molecular cancer therapeutics, 2014, Volume: 13, Issue:12 Topics: Animals; Biological Transport; Cell Line, Tumor; Cluster Analysis; Disease Models, Animal; Female; Glycolysis; Humans; Lactates; Metabolomics; Monocarboxylic Acid Transporters; Neoplasms; Oxidative Stress; Pyrimidinones; Radiation Tolerance; Symporters; Thiophenes; Tumor Burden; Xenograft Model Antitumor Assays	2014
Pharmacological targeting the ATR-CHK1-WEE1 axis involves balancing cell growth stimulation and apoptosis. Oncotarget, 2014, Nov-15, Volume: 5, Issue:21 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
Inhibition of Salmonella enterica biofilm formation using small-molecule adenosine mimetics. Antimicrobial agents and chemotherapy, 2015, Volume: 59, Issue:1 Topics: Acinetobacter baumannii; Adenosine; Adenosine Triphosphate; Anti-Bacterial Agents; Biofilms; Cell Line, Tumor; Chaperonin 60; Hep G2 Cells; Humans; Protein Binding; Pyrimidinones; Salmonella typhi; Salmonella typhimurium; Thiophenes	2015
A novel pyrido-thieno-pyrimidine derivative activates p53 through induction of phosphorylation and acetylation in colorectal cancer cells. International journal of oncology, 2015, Volume: 46, Issue:1 Topics: Acetylation; Antineoplastic Agents; Colorectal Neoplasms; G1 Phase Cell Cycle Checkpoints; Gene Expression Regulation, Neoplastic; HCT116 Cells; HT29 Cells; Humans; Phosphorylation; Protein Processing, Post-Translational; Pyrimidines; Pyrimidinones; Thiophenes; Tumor Suppressor Protein p53	2015
The discovery of a highly selective 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one SIRT2 inhibitor that is neuroprotective in an in vitro Parkinson's disease model. ChemMedChem, 2015, Volume: 10, Issue:1 Topics: Animals; Binding Sites; Cell Line; Cell Proliferation; Disease Models, Animal; Dopaminergic Neurons; Drug Evaluation, Preclinical; Forkhead Box Protein O3; Forkhead Transcription Factors; Histone Deacetylase Inhibitors; Humans; MCF-7 Cells; Molecular Docking Simulation; Neuroprotective Agents; Parkinson Disease; Protein Binding; Protein Structure, Tertiary; Pyrimidinones; Rats; Sirtuin 2; Structure-Activity Relationship; Thiophenes	2015
Novel Scaffold FingerPrint (SFP): applications in scaffold hopping and scaffold-based selection of diverse compounds. Journal of chemical information and modeling, 2015, Jan-26, Volume: 55, Issue:1 Topics: Computational Biology; Databases, Chemical; Databases, Factual; Drug Discovery; Hydrogen Bonding; Molecular Structure; Phosphodiesterase 5 Inhibitors; Proto-Oncogene Proteins B-raf; Pyrimidinones; Receptors, Somatostatin; Static Electricity; Structure-Activity Relationship; Thiophenes	2015
Pharmacological inhibition of BACE1 impairs synaptic plasticity and cognitive functions. Biological psychiatry, 2015, Apr-15, Volume: 77, Issue:8 Topics: Amyloid beta-Peptides; Amyloid Precursor Protein Secretases; Animals; Aspartic Acid Endopeptidases; Brain; Cognition; Cognitive Dysfunction; Dendritic Spines; Dose-Response Relationship, Drug; Enzyme Inhibitors; Exploratory Behavior; Humans; Maze Learning; Mice; Mice, Inbred C57BL; Mice, Transgenic; Peptide Fragments; Pyramidal Cells; Pyrimidines; Pyrimidinones; Synaptic Potentials; Thiazines; Thiophenes; Time Factors	2015
Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834. Bioorganic & medicinal chemistry letters, 2015, Mar-15, Volume: 25, Issue:6 Topics: Agammaglobulinaemia Tyrosine Kinase; Animals; Benzamides; Binding Sites; Bridged Bicyclo Compounds, Heterocyclic; Crystallography, X-Ray; Dogs; Half-Life; Humans; Mice; Microsomes, Liver; Molecular Dynamics Simulation; Protein Binding; Protein Kinase Inhibitors; Protein Structure, Tertiary; Protein-Tyrosine Kinases; Pyrimidinones; Rats; Structure-Activity Relationship; Thiophenes	2015
Conquering 2-aminopurine's deficiencies: highly emissive isomorphic guanosine surrogate faithfully monitors guanosine conformation and dynamics in DNA. Journal of the American Chemical Society, 2015, Mar-11, Volume: 137, Issue:9 Topics: 2-Aminopurine; Binding Sites; DNA, Viral; Fluorescence Polarization; Guanosine; HIV-1; Nucleic Acid Heteroduplexes; Pyrimidinones; Spectrometry, Fluorescence; Thiophenes	2015
An in vivo chemical genetic screen identifies phosphodiesterase 4 as a pharmacological target for hedgehog signaling inhibition. Cell reports, 2015, Apr-07, Volume: 11, Issue:1 Topics: Animals; Cyclic AMP-Dependent Protein Kinases; Cyclic Nucleotide Phosphodiesterases, Type 4; Hedgehog Proteins; Phosphodiesterase 4 Inhibitors; Pyrimidinones; Receptors, G-Protein-Coupled; Signal Transduction; Small Molecule Libraries; Smoothened Receptor; Thiophenes; Transcriptional Activation; Zebrafish; Zebrafish Proteins	2015
A novel reaction mediated by human aldehyde oxidase: amide hydrolysis of GDC-0834. Drug metabolism and disposition: the biological fate of chemicals, 2015, Volume: 43, Issue:6 Topics: Agammaglobulinaemia Tyrosine Kinase; Aldehyde Oxidase; Animals; Anti-Inflammatory Agents, Non-Steroidal; Biocatalysis; Catalytic Domain; Cytosol; Drug Stability; Drugs, Investigational; Gene Expression Profiling; Humans; Hydrolysis; Kinetics; Liver; Models, Molecular; Molecular Conformation; Molecular Docking Simulation; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrimidinones; Substrate Specificity; Thiophenes	2015
Optimisation of immunofluorescence methods to determine MCT1 and MCT4 expression in circulating tumour cells. BMC cancer, 2015, May-10, Volume: 15 Topics: Antineoplastic Agents; Cell Line, Tumor; Clinical Trials, Phase I as Topic; Fluorescent Antibody Technique; Healthy Volunteers; Humans; Monocarboxylic Acid Transporters; Muscle Proteins; Neoplastic Cells, Circulating; Pyrimidinones; Small Cell Lung Carcinoma; Symporters; Thiophenes	2015
Pharmacological inactivation of CHK1 and WEE1 induces mitotic catastrophe in nasopharyngeal carcinoma cells. Oncotarget, 2015, Aug-28, Volume: 6, Issue:25 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. BMC cancer, 2015, Jun-10, Volume: 15 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
Characterization of a mantle cell lymphoma cell line resistant to the Chk1 inhibitor PF-00477736. Oncotarget, 2015, Nov-10, Volume: 6, Issue:35 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
Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models. Journal of medicinal chemistry, 2015, Dec-24, Volume: 58, Issue:24 Topics: Adenosine A1 Receptor Antagonists; Adenosine A3 Receptor Antagonists; Animals; Binding, Competitive; CHO Cells; Computer Simulation; Cricetulus; High-Throughput Screening Assays; Humans; Ligands; Molecular Docking Simulation; Pyrimidinones; Receptor, Adenosine A1; Receptor, Adenosine A3; Sequence Homology, Amino Acid; Small Molecule Libraries; Structure-Activity Relationship; Thiazoles; Thiophenes	2015
Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability. Bioorganic & medicinal chemistry letters, 2016, Jan-15, Volume: 26, Issue:2 Topics: Agammaglobulinaemia Tyrosine Kinase; Animals; Dogs; Humans; Mice; Microsomes, Liver; Models, Molecular; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyridazines; Pyrimidinones; Rats; Thiophenes	2016
MCT1 Modulates Cancer Cell Pyruvate Export and Growth of Tumors that Co-express MCT1 and MCT4. Cell reports, 2016, Feb-23, Volume: 14, Issue:7 Topics: Animals; Antineoplastic Agents; Biological Transport; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Citric Acid Cycle; Epithelial Cells; Female; Gene Expression Profiling; Gene Expression Regulation, Neoplastic; Glycolysis; Humans; Lung Neoplasms; Mice; Monocarboxylic Acid Transporters; Muscle Proteins; Oxidative Phosphorylation; Pyrimidinones; Pyruvic Acid; Signal Transduction; Symporters; Thiophenes; Tumor Burden; Xenograft Model Antitumor Assays	2016
Constant pH Molecular Dynamics Reveals pH-Modulated Binding of Two Small-Molecule BACE1 Inhibitors. The journal of physical chemistry letters, 2016, Mar-17, Volume: 7, Issue:6 Topics: Amyloid beta-Peptides; Amyloid Precursor Protein Secretases; Animals; Aspartic Acid Endopeptidases; Caco-2 Cells; Hepatocytes; Humans; Hydrogen-Ion Concentration; Molecular Dynamics Simulation; Peptide Fragments; Protease Inhibitors; Pyrimidinones; Rats; Thiophenes	2016
Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats. Proceedings of the National Academy of Sciences of the United States of America, 2016, Mar-29, Volume: 113, Issue:13 Topics: Acetyl-CoA Carboxylase; Animals; Dyslipidemias; Enzyme Inhibitors; Fatty Liver; Female; Hep G2 Cells; Humans; Insulin Resistance; Male; Molecular Docking Simulation; Obesity; Protein Multimerization; Pyrimidinones; Rats, Sprague-Dawley; Rats, Zucker; Structure-Activity Relationship; Thiophenes	2016
Simple approach to thieno[3,2-d]pyrimidines as new scaffolds of antimicrobial activities. Acta pharmaceutica (Zagreb, Croatia), 2016, Sep-01, Volume: 66, Issue:3 Topics: Anti-Bacterial Agents; Antifungal Agents; Aspergillus flavus; Candida albicans; Drug Design; Ganoderma; Gram-Negative Bacteria; Gram-Positive Bacteria; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Pyrimidines; Pyrimidinones; Spiro Compounds; Stereoisomerism; Structure-Activity Relationship; Thiophenes; Transition Temperature	2016
Discovery of a potent and highly selective transforming growth factor β receptor-associated kinase 1 (TAK1) inhibitor by structure based drug design (SBDD). Bioorganic & medicinal chemistry, 2016, 09-15, Volume: 24, Issue:18 Topics: Animals; Asparagine; Crystallography, X-Ray; Drug Design; Enzyme Assays; Humans; Hydrogen Bonding; MAP Kinase Kinase Kinases; Mice; Microsomes, Liver; Molecular Structure; Protein Kinase Inhibitors; Pyrimidinones; Serine; Solubility; Structure-Activity Relationship; Thiophenes; Tyrosine	2016
Identification of the first small-molecule inhibitor of the REV7 DNA repair protein interaction. Bioorganic & medicinal chemistry, 2016, 09-15, Volume: 24, Issue:18 Topics: Antineoplastic Agents; Cisplatin; DNA Repair; DNA-Binding Proteins; DNA-Directed DNA Polymerase; Drug Resistance, Neoplasm; HeLa Cells; Humans; Mad2 Proteins; Protein Binding; Pyrimidinones; Structure-Activity Relationship; Thiophenes	2016
Melanin-Concentrating Hormone and Its MCH-1 Receptor: Relationship Between Effects on Alcohol and Caloric Intake. Alcoholism, clinical and experimental research, 2016, Volume: 40, Issue:10 Topics: Alcohol Drinking; Animals; Eating; Energy Intake; Gene Expression; Hypothalamic Hormones; Hypothalamus; Male; Melanins; Motivation; Nucleus Accumbens; Pituitary Hormones; Pyrimidinones; Rats; Receptors, Somatostatin; Self Administration; Thiophenes	2016
Inactivation of the melanin concentrating hormone system impairs maternal behavior. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology, 2016, Volume: 26, Issue:11 Topics: Aggression; Animals; Animals, Newborn; Cannibalism; Female; Gene Expression Regulation; Genes, fos; Lactation; Maternal Behavior; Mice; Mice, Knockout; Nesting Behavior; Prolactin; Pyrimidinones; Receptors, Somatostatin; Thiophenes	2016
Inhibition of acetyl-CoA carboxylase suppresses fatty acid synthesis and tumor growth of non-small-cell lung cancer in preclinical models. Nature medicine, 2016, Volume: 22, Issue:10 Topics: Acetyl-CoA Carboxylase; Acetyltransferases; Allosteric Regulation; AMP-Activated Protein Kinases; Animals; Carcinoma, Non-Small-Cell Lung; Cell Proliferation; Enzyme Inhibitors; Fatty Acids; Humans; Lipid Metabolism; Lung Neoplasms; Mice; Mice, Knockout; Molecular Targeted Therapy; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins p21(ras); Pyrimidinones; Thiophenes; Tumor Suppressor Protein p53; Xenograft Model Antitumor Assays	2016
MEK inhibitors block growth of lung tumours with mutations in ataxia-telangiectasia mutated. Nature communications, 2016, 12-06, Volume: 7 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
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach. Journal of medicinal chemistry, 2017, 01-26, Volume: 60, Issue:2 Topics: Animals; Cartilage; Cattle; Chelating Agents; Collagen; Drug Design; Matrix Metalloproteinase 13; Matrix Metalloproteinase Inhibitors; Pyrimidines; Pyrimidinones; Quinazolines; Thiophenes; Triazoles; Zinc	2017
Neurotoxicity of a Biopesticide Analog on Zebrafish Larvae at Nanomolar Concentrations. International journal of molecular sciences, 2016, Dec-19, Volume: 17, Issue:12 Topics: Animals; Apoptosis; Biological Control Agents; Cell Proliferation; Endocrine Disruptors; Gene Expression Regulation; Larva; Lateral Line System; Mechanoreceptors; Nerve Regeneration; Pyrimidines; Pyrimidinones; Receptors, Estrogen; Spinal Cord; Thiophenes; Zebrafish	2016
Inhibition of CHK1 and WEE1 as a new therapeutic approach in diffuse large B cell lymphomas with MYC deregulation. British journal of haematology, 2018, Volume: 181, Issue:1 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. Oncotarget, 2017, Feb-14, Volume: 8, Issue:7 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
HPLC-UV method for simultaneous determination of MK-1775 and AZD-7762 in both acetonitrile-aqueous solution and mouse plasma. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 2017, Feb-15, Volume: 1044-1045 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. Cancer letters, 2017, 04-28, Volume: 392 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
MACC1 mediates chemotherapy sensitivity of 5-FU and cisplatin via regulating MCT1 expression in gastric cancer. Biochemical and biophysical research communications, 2017, 04-08, Volume: 485, Issue:3 Topics: Antineoplastic Agents; Blotting, Western; Cell Line, Tumor; Cell Survival; Cisplatin; Female; Fluorouracil; Gene Expression Regulation, Neoplastic; Humans; Kaplan-Meier Estimate; Male; Middle Aged; Monocarboxylic Acid Transporters; Multivariate Analysis; Prognosis; Pyrimidinones; Reverse Transcriptase Polymerase Chain Reaction; RNA Interference; Stomach Neoplasms; Symporters; Thiophenes; Trans-Activators; Transcription Factors	2017
Inhibition of monocarboxyate transporter 1 by AZD3965 as a novel therapeutic approach for diffuse large B-cell lymphoma and Burkitt lymphoma. Haematologica, 2017, Volume: 102, Issue:7 Topics: Antineoplastic Agents; Biomarkers; Burkitt Lymphoma; Cell Death; Cell Line, Tumor; Drug Resistance, Neoplasm; Electron Transport Complex I; Energy Metabolism; Humans; Lactic Acid; Lymphoma, Large B-Cell, Diffuse; Mitochondria; Monocarboxylic Acid Transporters; Muscle Proteins; Oxidative Phosphorylation; Pyrimidinones; Symporters; Thiophenes	2017
2-Aminomethylthieno[3,2-d]pyrimidin-4(3H)-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time-dependent inhibitors of Cdc7 kinase. Bioorganic & medicinal chemistry, 2017, 07-15, Volume: 25, Issue:14 Topics: Binding Sites; Cell Cycle Proteins; Cyclin-Dependent Kinase 2; Humans; Inhibitory Concentration 50; Kinetics; Molecular Docking Simulation; Protein Binding; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Protein Structure, Tertiary; Pyrazoles; Pyrimidinones; Recombinant Proteins; rho-Associated Kinases; Structure-Activity Relationship; Thiophenes	2017
Gli1-labeled adult mesenchymal stem/progenitor cells and hedgehog signaling contribute to endochondral heterotopic ossification. Bone, 2018, Volume: 109 Topics: Animals; Hedgehog Proteins; Mesenchymal Stem Cells; Mice; Mice, Transgenic; Ossification, Heterotopic; Osteogenesis; Pyrimidinones; Signal Transduction; Thiophenes; Zinc Finger Protein GLI1	2018
Melanin concentrating hormone modulates oxytocin-mediated marble burying. Neuropharmacology, 2018, Volume: 128 Topics: Adaptation, Ocular; Analysis of Variance; Animals; Diphtheria Toxin; Exploratory Behavior; Glycoproteins; Green Fluorescent Proteins; Grooming; Hypothalamic Hormones; Luminescent Proteins; Male; Maze Learning; Melanins; Mice; Mice, Inbred C57BL; Mice, Transgenic; Motor Activity; Oxytocin; Pituitary Hormones; Pyrimidinones; Receptors, Oxytocin; Receptors, Somatostatin; Red Fluorescent Protein; Stereotyped Behavior; Thiophenes	2018
MCT1 Inhibitor AZD3965 Increases Mitochondrial Metabolism, Facilitating Combination Therapy and Noninvasive Magnetic Resonance Spectroscopy. Cancer research, 2017, 11-01, Volume: 77, Issue:21 Topics: Acrylates; Animals; Antineoplastic Combined Chemotherapy Protocols; Blotting, Western; Cell Line, Tumor; Energy Metabolism; Female; HT29 Cells; Humans; Lactic Acid; Lymphoma; Magnetic Resonance Spectroscopy; Metformin; Mice, SCID; Mitochondria; Monocarboxylic Acid Transporters; Muscle Proteins; Pyrimidinones; Symporters; Thiophenes; Xenograft Model Antitumor Assays	2017
Design, synthesis and biological evaluations of N-Hydroxy thienopyrimidine-2,4-diones as inhibitors of HIV reverse transcriptase-associated RNase H. European journal of medicinal chemistry, 2017, Dec-01, Volume: 141 Topics: Antiviral Agents; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Design; HIV; HIV Reverse Transcriptase; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Pyrimidinones; Reverse Transcriptase Inhibitors; Ribonuclease H, Human Immunodeficiency Virus; Structure-Activity Relationship; Thiophenes	2017
Fluorescent-Linked Enzyme Chemoproteomic Strategy (FLECS) for Identifying HSP70 Inhibitors. Methods in molecular biology (Clifton, N.J.), 2018, Volume: 1709 Topics: Animals; Heat-Shock Response; HSP70 Heat-Shock Proteins; Humans; Proteomics; Pyrazoles; Pyrimidines; Pyrimidinones; Signal Transduction; Thiophenes	2018
A simple and sensitive HPLC-MS/MS method for quantification of eggmanone in rat plasma and its application to pharmacokinetics. Journal of pharmaceutical and biomedical analysis, 2018, May-10, Volume: 153 Topics: Animals; Calibration; Chromatography, High Pressure Liquid; Female; Male; Phosphodiesterase 4 Inhibitors; Plasma; Pyrimidinones; Rats; Rats, Sprague-Dawley; Reproducibility of Results; Sensitivity and Specificity; Tandem Mass Spectrometry; Thiophenes	2018
Development and validation of a liquid chromatography tandem mass spectrometry assay for AZD3965 in mouse plasma and tumor tissue: Application to pharmacokinetic and breast tumor xenograft studies. Journal of pharmaceutical and biomedical analysis, 2018, Jun-05, Volume: 155 Topics: Acetonitriles; Animals; Atmospheric Pressure; Breast Neoplasms; Cell Line, Tumor; Chromatography, Liquid; Female; Heterografts; Mice; Plasma; Pyrimidines; Pyrimidinones; Reproducibility of Results; Tandem Mass Spectrometry; Thiophenes; Uracil	2018
Clinical resistance associated with a novel MAP2K1 mutation in a patient with Langerhans cell histiocytosis. Pediatric blood & cancer, 2018, Volume: 65, Issue:9 Topics: Adolescent; Adrenal Cortex Hormones; Butadienes; Combined Modality Therapy; Cytarabine; Disease Progression; Drug Resistance; Drug Therapy, Combination; Enzyme Activation; Exons; HEK293 Cells; Hematopoietic Stem Cell Transplantation; Histiocytosis, Langerhans-Cell; Humans; Male; MAP Kinase Kinase 1; MAP Kinase Signaling System; Molecular Targeted Therapy; Mutation; Nitriles; Protein Kinase Inhibitors; Proto-Oncogene Proteins B-raf; Pyrazoles; Pyridones; Pyrimidinones; Recombinant Fusion Proteins; Sequence Deletion; Thiophenes; Vincristine	2018
Detection of Chemical Engagement of Solute Carrier Proteins by a Cellular Thermal Shift Assay. ACS chemical biology, 2018, 06-15, Volume: 13, Issue:6 Topics: Biological Assay; Excitatory Amino Acid Transporter 2; Formates; Glutamate Plasma Membrane Transport Proteins; Heating; HEK293 Cells; Humans; Lactic Acid; Ligands; Monocarboxylic Acid Transporters; Protein Binding; Protein Stability; Pyrimidinones; Thiophenes; Uracil	2018
Extending Remission and Reversing New-Onset Type 1 Diabetes by Targeted Ablation of Autoreactive T Cells. Diabetes, 2018, Volume: 67, Issue:11 Topics: Animals; Diabetes Mellitus, Type 1; Enzyme Inhibitors; Imidazoles; Mice; Mice, Inbred NOD; Pancreas; Piperazines; Pyrazoles; Pyrimidines; Pyrimidinones; T-Lymphocytes; Thiophenes; Urea	2018
Statin-induced metabolic reprogramming in head and neck cancer: a biomarker for targeting monocarboxylate transporters. Scientific reports, 2018, 11-14, Volume: 8, Issue:1 Topics: Animals; Biomarkers; Head and Neck Neoplasms; Humans; Hydroxymethylglutaryl-CoA Reductase Inhibitors; Lactic Acid; Mice; Monocarboxylic Acid Transporters; Oxidative Phosphorylation; Precision Medicine; Prognosis; Pyrimidinones; Thiophenes	2018
Acetaminophen cytotoxicity in HepG2 cells is associated with a decoupling of glycolysis from the TCA cycle, loss of NADPH production, and suppression of anabolism. Archives of toxicology, 2019, Volume: 93, Issue:2 Topics: Acetaminophen; Cell Survival; Citric Acid Cycle; Drug Synergism; Glutathione; Glycolysis; Hep G2 Cells; Humans; Lactates; Metabolism; Monocarboxylic Acid Transporters; NADP; Pyrimidinones; Symporters; Thiophenes; Toxicity Tests	2019
Cellular Uptake of MCT1 Inhibitors AR-C155858 and AZD3965 and Their Effects on MCT-Mediated Transport of L-Lactate in Murine 4T1 Breast Tumor Cancer Cells. The AAPS journal, 2019, 01-07, Volume: 21, Issue:2 Topics: Animals; Breast Neoplasms; Cell Line, Tumor; Coumaric Acids; Drug Screening Assays, Antitumor; Female; Humans; Hydrogen-Ion Concentration; Lactic Acid; Mice; Monocarboxylic Acid Transporters; Pyrimidinones; Symporters; Thiophenes; Uracil	2019
Clinical significance of metabolism-related biomarkers in non-Hodgkin lymphoma - MCT1 as potential target in diffuse large B cell lymphoma. Cellular oncology (Dordrecht), 2019, Volume: 42, Issue:3 Topics: Adult; Aged; Aged, 80 and over; Biomarkers, Tumor; Cell Line, Tumor; Cell Survival; Female; Glycolysis; Humans; Kaplan-Meier Estimate; Lymphoma, Large B-Cell, Diffuse; Lymphoma, Non-Hodgkin; Male; Middle Aged; Monocarboxylic Acid Transporters; Pyrimidinones; Symporters; Thiophenes; Young Adult	2019
Inhibition of seryl tRNA synthetase by seryl nucleoside moiety (SB-217452) of albomycin antibiotic. Journal of biomolecular structure & dynamics, 2020, Volume: 38, Issue:8 Topics: Anti-Bacterial Agents; Ferrichrome; Nucleosides; Pyrimidinones; Serine-tRNA Ligase; Thiophenes	2020
Synthesis and anti-cancer activity of ND-646 and its derivatives as acetyl-CoA carboxylase 1 inhibitors. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 2019, Sep-01, Volume: 137 Topics: Acetyl-CoA Carboxylase; Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Humans; Lung Neoplasms; Pyrimidinones; RNA, Messenger; Thiophenes	2019
Utilization of tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinone as a cap moiety in design of novel histone deacetylase inhibitors. Bioorganic chemistry, 2019, Volume: 91 Topics: Antineoplastic Agents; Apoptosis; Catalytic Domain; Cell Line, Tumor; Cell Proliferation; Chelating Agents; Drug Design; Drug Screening Assays, Antitumor; G2 Phase Cell Cycle Checkpoints; Histone Deacetylase 1; Histone Deacetylase 2; Histone Deacetylase Inhibitors; Humans; Hydroxamic Acids; Molecular Docking Simulation; Molecular Structure; Protein Binding; Pyrimidinones; Structure-Activity Relationship; Thiophenes; Zinc	2019
A pharmacogenomic analysis using L1000CDS Cancer letters, 2019, Nov-28, Volume: 465 Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Pancreatic Ductal; Cell Line, Tumor; Cell Movement; Cell Proliferation; Cell Survival; Gene Expression Regulation, Neoplastic; Glycogen Synthase Kinase 3 beta; Humans; Inhibitory Concentration 50; Male; Mice; Pancreatic Neoplasms; Pharmacogenomic Testing; Pyridones; Pyrimidines; Pyrimidinones; Signal Transduction; Thiophenes; TOR Serine-Threonine Kinases; Xenograft Model Antitumor Assays	2019
A Nonradioactive High-Throughput Screening-Compatible Cell-Based Assay to Identify Inhibitors of the Monocarboxylate Transporter Protein 1. Assay and drug development technologies, 2019, Volume: 17, Issue:6 Topics: Animals; Cell Survival; Cells, Cultured; HEK293 Cells; High-Throughput Screening Assays; Humans; Mice; Molecular Structure; Monocarboxylic Acid Transporters; Pyrimidinones; Pyruvates; Symporters; Thiophenes	2019
Pharmacokinetics of the Monocarboxylate Transporter 1 Inhibitor AZD3965 in Mice: Potential Enterohepatic Circulation and Target-Mediated Disposition. Pharmaceutical research, 2019, Dec-10, Volume: 37, Issue:1 Topics: Administration, Oral; Animals; Chromatography, High Pressure Liquid; Delayed-Action Preparations; Drug Delivery Systems; Enterohepatic Circulation; Female; Glucuronides; Humans; Mice; Mice, Inbred BALB C; Pyrimidinones; Tandem Mass Spectrometry; Thiophenes; Tissue Distribution	2019
Identification of the Enzymes Mediating the Maturation of the Seryl-tRNA Synthetase Inhibitor SB-217452 during the Biosynthesis of Albomycins. Angewandte Chemie (International ed. in English), 2020, 02-24, Volume: 59, Issue:9 Topics: Anti-Bacterial Agents; Biocatalysis; Ferrichrome; Peptide Synthases; Pyrimidinones; Serine-tRNA Ligase; Streptomyces; Thiophenes	2020
Discovery of a Novel, Highly Potent, and Selective Thieno[3,2- Journal of medicinal chemistry, 2020, 02-13, Volume: 63, Issue:3 Topics: Animals; Antineoplastic Agents; Binding Sites; Cell Cycle Proteins; Cell Line, Tumor; Drug Design; Drug Discovery; Formaldehyde; Humans; Mice; Molecular Docking Simulation; Molecular Structure; Protein Binding; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Pyrazolones; Pyrimidines; Pyrimidinones; Quinuclidines; Structure-Activity Relationship; Thiophenes; Xenograft Model Antitumor Assays	2020
Monocarboxylate transporter 1 blockade with AZD3965 inhibits lipid biosynthesis and increases tumour immune cell infiltration. British journal of cancer, 2020, Volume: 122, Issue:6 Topics: Animals; Cell Culture Techniques; Cell Line; Cell Line, Tumor; Disease Models, Animal; Female; Humans; Lipid Metabolism; Mice; Monocarboxylic Acid Transporters; Pyrimidinones; Thiophenes	2020
Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones. European journal of medicinal chemistry, 2020, Mar-01, Volume: 189 Topics: Angiogenesis Inhibitors; Animals; Binding Sites; CDC2 Protein Kinase; Cell Line, Tumor; Cell Proliferation; Chickens; Drug Screening Assays, Antitumor; G2 Phase Cell Cycle Checkpoints; Humans; Molecular Docking Simulation; Molecular Structure; Protein Binding; Protein Kinase Inhibitors; Pyrimidinones; Structure-Activity Relationship; Swine; Thiophenes; Tubulin; Tubulin Modulators; Zebrafish	2020
A case of malignant hyperlactaemic acidosis appearing upon treatment with the mono-carboxylase transporter 1 inhibitor AZD3965. British journal of cancer, 2020, Volume: 122, Issue:8 Topics: Acidosis, Lactic; Humans; Hyperlactatemia; Male; Melanoma; Middle Aged; Monocarboxylic Acid Transporters; Positron-Emission Tomography; Pyrimidinones; Symporters; Thiophenes	2020
PEGylated PLGA Nanoparticle Delivery of Eggmanone for T Cell Modulation: Applications in Rheumatic Autoimmunity. International journal of nanomedicine, 2020, Volume: 15 Topics: Animals; Autoimmunity; CD4-Positive T-Lymphocytes; Cytokines; Drug Delivery Systems; Female; Hedgehog Proteins; Immunoglobulin Fragments; Immunologic Factors; Mice, Inbred C57BL; Nanoparticles; Polylactic Acid-Polyglycolic Acid Copolymer; Pyrimidinones; Rheumatic Diseases; T-Lymphocytes; T-Lymphocytes, Helper-Inducer; Thiophenes	2020
Discovery of New Apoptosis-Inducing Agents for Breast Cancer Based on Ethyl 2-Amino-4,5,6,7-Tetra Hydrobenzo[ Molecules (Basel, Switzerland), 2020, May-28, Volume: 25, Issue:11 Topics: Alkylation; Antineoplastic Agents; Apoptosis; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Hep G2 Cells; Humans; MCF-7 Cells; Pyrimidinones; Structure-Activity Relationship; Thiophenes	2020
In Vitro and In Vivo Efficacy of AZD3965 and Alpha-Cyano-4-Hydroxycinnamic Acid in the Murine 4T1 Breast Tumor Model. The AAPS journal, 2020, 06-11, Volume: 22, Issue:4 Topics: Animals; Breast Neoplasms; Cell Line, Tumor; Coumaric Acids; Dose-Response Relationship, Drug; Female; Lung Neoplasms; Mice; Mice, Inbred BALB C; Monocarboxylic Acid Transporters; Pyrimidinones; Symporters; Thiophenes; Treatment Outcome; Tumor Burden; Xenograft Model Antitumor Assays	2020
Effects of a monocarboxylate transport 1 inhibitor, AZD3965, on retinal and visual function in the rat. British journal of pharmacology, 2020, Volume: 177, Issue:20 Topics: Animals; Electroretinography; Pyrimidinones; Rats; Rats, Long-Evans; Rats, Wistar; Retina; Thiophenes	2020
Scaffold hopping and optimisation of 3',4'-dihydroxyphenyl- containing thienopyrimidinones: synthesis of quinazolinone derivatives as novel allosteric inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H. Journal of enzyme inhibition and medicinal chemistry, 2020, Volume: 35, Issue:1 Topics: Anti-HIV Agents; Catalytic Domain; Drug Design; HIV Reverse Transcriptase; Humans; Models, Molecular; Protein Binding; Protein Multimerization; Pyrimidinones; Quinazolinones; Reverse Transcriptase Inhibitors; Ribonuclease H, Human Immunodeficiency Virus; Structure-Activity Relationship; Thiophenes	2020
Structural basis of human monocarboxylate transporter 1 inhibition by anti-cancer drug candidates. Cell, 2021, 01-21, Volume: 184, Issue:2 Topics: Amino Acid Sequence; Animals; Antineoplastic Agents; Basigin; Binding Sites; Cryoelectron Microscopy; Humans; Ligands; Models, Molecular; Monocarboxylic Acid Transporters; Mutant Proteins; Protons; Pyrimidinones; Rats; Structural Homology, Protein; Substrate Specificity; Symporters; Thiophenes	2021
Catastrophic ATP loss underlies a metabolic combination therapy tailored for Proceedings of the National Academy of Sciences of the United States of America, 2021, 03-30, Volume: 118, Issue:13 Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Basigin; Cell Line, Tumor; Cell Proliferation; Electron Transport Complex I; Gene Amplification; Humans; Mice; Mitochondria; Monocarboxylic Acid Transporters; N-Myc Proto-Oncogene Protein; Neuroblastoma; Phenformin; Pyrimidinones; Symporters; Thiophenes; Xenograft Model Antitumor Assays	2021
A Holistic Evolutionary and 3D Pharmacophore Modelling Study Provides Insights into the Metabolism, Function, and Substrate Selectivity of the Human Monocarboxylate Transporter 4 (hMCT4). International journal of molecular sciences, 2021, Mar-13, Volume: 22, Issue:6 Topics: Animals; Antineoplastic Agents; Binding Sites; Biological Transport; Drug Design; Glycolysis; Humans; Lactic Acid; Molecular Docking Simulation; Monocarboxylic Acid Transporters; Muscle Proteins; Phloretin; Phylogeny; Protein Binding; Protein Conformation, alpha-Helical; Protein Interaction Domains and Motifs; Protein Isoforms; Pyrimidinones; Quercetin; Reserpine; Structural Homology, Protein; Substrate Specificity; Thiophenes; Uracil	2021
Targeting neovascularization and respiration of tumor grafts grown on chick embryo chorioallantoic membranes. PloS one, 2021, Volume: 16, Issue:5 Topics: Angiogenesis Inhibitors; Animals; Cell Line, Tumor; Chick Embryo; Chorioallantoic Membrane; Dogs; Humans; Mice; Monocarboxylic Acid Transporters; Neoplasm Proteins; Neoplasms, Experimental; Neovascularization, Pathologic; Oxygen Consumption; Pyrimidinones; Symporters; Thiophenes; Xenograft Model Antitumor Assays	2021
Multifunctional Spiky Topological Nanocapsules for the Discrimination and Differential Inhibition of Inflammation and Cancer. ACS applied materials & interfaces, 2021, Jun-09, Volume: 13, Issue:22 Topics: Animals; Apoptosis; Carcinoma, Hepatocellular; Cell Movement; Cell Proliferation; Drug Liberation; Female; Humans; Inflammation; Liver Neoplasms; Mice; Mice, Inbred BALB C; Mice, Nude; MicroRNAs; Monocarboxylic Acid Transporters; Nanocapsules; Pyrimidinones; Symporters; Thiophenes; Tumor Cells, Cultured; Xenograft Model Antitumor Assays	2021
Regulation of Brain Primary Cilia Length by MCH Signaling: Evidence from Pharmacological, Genetic, Optogenetic, and Chemogenic Manipulations. Molecular neurobiology, 2022, Volume: 59, Issue:1 Topics: Animals; Caudate Nucleus; Cilia; Hypothalamic Hormones; Melanins; Mice; Mice, Knockout; Neurons; Optogenetics; Pituitary Hormones; Prefrontal Cortex; Pyrimidinones; Rats; Rats, Wistar; Receptors, Somatostatin; Thiophenes	2022
Metabolic drug survey highlights cancer cell dependencies and vulnerabilities. Nature communications, 2021, 12-14, Volume: 12, Issue:1 Topics: Biomarkers, Tumor; Cell Survival; Cluster Analysis; Fatty Acids; Genotype; Humans; Leukemia, Myeloid; Monocarboxylic Acid Transporters; Phenotype; Phosphatidylinositol 3-Kinase; Phosphoinositide-3 Kinase Inhibitors; Pyrimidinones; Pyrrolidines; Signal Transduction; Small Molecule Libraries; Symporters; Systems Analysis; Thiophenes; Triazoles; Tumor Cells, Cultured	2021
Novel and conventional inhibitors of canonical autophagy differently affect LC3-associated phagocytosis. FEBS letters, 2022, Volume: 596, Issue:4 Topics: Autophagosomes; Autophagy; Cell Differentiation; Chloroquine; Class III Phosphatidylinositol 3-Kinases; Dendritic Cells; Endosomes; Gene Expression Regulation; Humans; Lysosomes; Macrolides; Microtubule-Associated Proteins; Monocytes; Phagocytosis; Phagosomes; Primary Cell Culture; Proteasome Endopeptidase Complex; Pyridines; Pyrimidinones; Thiophenes; Zymosan	2022
Inhibition of the Monocarboxylate Transporter 1 (MCT1) Promotes 3T3-L1 Adipocyte Proliferation and Enhances Insulin Sensitivity. International journal of molecular sciences, 2022, Feb-08, Volume: 23, Issue:3 Topics: 3T3-L1 Cells; Adipocytes; Animals; CDC2 Protein Kinase; Cell Cycle; Cell Proliferation; Down-Regulation; Glucose; Insulin Resistance; Mice; Models, Biological; Monocarboxylic Acid Transporters; Pyrimidinones; Symporters; Thiophenes	2022