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Items: 1 to 20 of 134

1.

Analogues of 4-[(7-Bromo-2-methyl-4-oxo-3H-quinazolin-6-yl)methylprop-2-ynylamino]-N-(3-pyridylmethyl)benzamide (CB-30865) as potent inhibitors of nicotinamide phosphoribosyltransferase (Nampt).

Lockman JW, Murphy BR, Zigar DF, Judd WR, Slattum PM, Gao ZH, Ostanin K, Green J, McKinnon R, Terry-Lorenzo RT, Fleischer TC, Boniface JJ, Shenderovich M, Willardsen JA.

J Med Chem. 2010 Dec 23;53(24):8734-46. doi: 10.1021/jm101145b. Epub 2010 Nov 16.

PMID:
21080724
2.

Chemical proteomics identifies Nampt as the target of CB30865, an orphan cytotoxic compound.

Fleischer TC, Murphy BR, Flick JS, Terry-Lorenzo RT, Gao ZH, Davis T, McKinnon R, Ostanin K, Willardsen JA, Boniface JJ.

Chem Biol. 2010 Jun 25;17(6):659-64. doi: 10.1016/j.chembiol.2010.05.008.

3.

The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent.

Bavetsias V, Skelton LA, Yafai F, Mitchell F, Wilson SC, Allan B, Jackman AL.

J Med Chem. 2002 Aug 15;45(17):3692-702.

PMID:
12166942
4.

Carboranes increase the potency of small molecule inhibitors of nicotinamide phosphoribosyltranferase.

Lee MW Jr, Sevryugina YV, Khan A, Ye SQ.

J Med Chem. 2012 Aug 23;55(16):7290-4. doi: 10.1021/jm300740t. Epub 2012 Aug 13.

PMID:
22889195
5.

Quinazoline antifolate thymidylate synthase inhibitors: replacement of glutamic acid in the C2-methyl series.

Marsham PR, Jackman AL, Barker AJ, Boyle FT, Pegg SJ, Wardleworth JM, Kimbell R, O'Connor BM, Calvert AH, Hughes LR.

J Med Chem. 1995 Mar 17;38(6):994-1004.

PMID:
7699716
6.

Structure-based design of substituted diphenyl sulfones and sulfoxides as lipophilic inhibitors of thymidylate synthase.

Jones TR, Webber SE, Varney MD, Reddy MR, Lewis KK, Kathardekar V, Mazdiyasni H, Deal J, Nguyen D, Welsh KM, Webber S, Johnston A, Matthews DA, Smith WW, Janson CA, Bacquet RJ, Howland EF, Booth CL, Herrmann SM, Ward RW, White J, Bartlett CA, Morse CA.

J Med Chem. 1997 Feb 28;40(5):677-83.

PMID:
9057854
7.

Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Giannetti AM, Zheng X, Skelton NJ, Wang W, Bravo BJ, Bair KW, Baumeister T, Cheng E, Crocker L, Feng Y, Gunzner-Toste J, Ho YC, Hua R, Liederer BM, Liu Y, Ma X, O'Brien T, Oeh J, Sampath D, Shen Y, Wang C, Wang L, Wu H, Xiao Y, Yuen PW, Zak M, Zhao G, Zhao Q, Dragovich PS.

J Med Chem. 2014 Feb 13;57(3):770-92. doi: 10.1021/jm4015108. Epub 2014 Jan 22.

PMID:
24405419
8.

Structure-based design of lipophilic quinazoline inhibitors of thymidylate synthase.

Jones TR, Varney MD, Webber SE, Lewis KK, Marzoni GP, Palmer CL, Kathardekar V, Welsh KM, Webber S, Matthews DA, Appelt K, Smith WW, Janson CA, Villafranca JE, Bacquet RJ, Howland EF, Booth CL, Herrmann SM, Ward RW, White J, Moomaw EW, Bartlett CA, Morse CA.

J Med Chem. 1996 Feb 16;39(4):904-17.

PMID:
8632414
9.

Structural and biochemical analyses of the catalysis and potency impact of inhibitor phosphoribosylation by human nicotinamide phosphoribosyltransferase.

Oh A, Ho YC, Zak M, Liu Y, Chen X, Yuen PW, Zheng X, Liu Y, Dragovich PS, Wang W.

Chembiochem. 2014 May 26;15(8):1121-30. doi: 10.1002/cbic.201402023. Epub 2014 May 5.

PMID:
24797455
10.

Nicotinamide phosphoribosyltransferase inhibitors, design, preparation, and structure-activity relationship.

Christensen MK, Erichsen KD, Olesen UH, Tjørnelund J, Fristrup P, Thougaard A, Nielsen SJ, Sehested M, Jensen PB, Loza E, Kalvinsh I, Garten A, Kiess W, Björkling F.

J Med Chem. 2013 Nov 27;56(22):9071-88. doi: 10.1021/jm4009949. Epub 2013 Nov 13.

PMID:
24164086
11.

A fluorometric assay for high-throughput screening targeting nicotinamide phosphoribosyltransferase.

Zhang RY, Qin Y, Lv XQ, Wang P, Xu TY, Zhang L, Miao CY.

Anal Biochem. 2011 May 1;412(1):18-25. doi: 10.1016/j.ab.2010.12.035. Epub 2011 Jan 4.

PMID:
21211508
12.

Fragment-based design of 3-aminopyridine-derived amides as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Dragovich PS, Zhao G, Baumeister T, Bravo B, Giannetti AM, Ho YC, Hua R, Li G, Liang X, Ma X, O'Brien T, Oh A, Skelton NJ, Wang C, Wang W, Wang Y, Xiao Y, Yuen PW, Zak M, Zhao Q, Zheng X.

Bioorg Med Chem Lett. 2014 Feb 1;24(3):954-62. doi: 10.1016/j.bmcl.2013.12.062. Epub 2013 Dec 21.

PMID:
24433859
13.

Substituted quinazolines, part 2. Synthesis and in-vitro anticancer evaluation of new 2-substituted mercapto-3H-quinazoline analogs.

Khalil AA, Abdel-Hamide SG, Al-Obaid AM, El-Subbagh HI.

Arch Pharm (Weinheim). 2003 Apr;336(2):95-103.

PMID:
12761762
14.

Target enzyme mutations are the molecular basis for resistance towards pharmacological inhibition of nicotinamide phosphoribosyltransferase.

Olesen UH, Petersen JG, Garten A, Kiess W, Yoshino J, Imai S, Christensen MK, Fristrup P, Thougaard AV, Björkling F, Jensen PB, Nielsen SJ, Sehested M.

BMC Cancer. 2010 Dec 12;10:677. doi: 10.1186/1471-2407-10-677.

15.

Synthesis, antitubercular and anticancer activities of substituted furyl-quinazolin-3(4H)-ones.

Raghavendra NM, Thampi P, Gurubasavarajaswamy PM, Sriram D.

Arch Pharm (Weinheim). 2007 Dec;340(12):635-41.

PMID:
17994604
16.

Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors.

Liu LT, Yuan TT, Liu HH, Chen SF, Wu YT.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6373-7. Epub 2007 Aug 28.

PMID:
17889528
17.

Structure-based design and synthesis of lipophilic 2,4-diamino-6-substituted quinazolines and their evaluation as inhibitors of dihydrofolate reductases and potential antitumor agents.

Gangjee A, Vidwans AP, Vasudevan A, Queener SF, Kisliuk RL, Cody V, Li R, Galitsky N, Luft JR, Pangborn W.

J Med Chem. 1998 Aug 27;41(18):3426-34.

PMID:
9719595
19.

Synthesis and antitumor activities evaluation of m-(4-morpholinoquinazolin-2-yl)benzamides in vitro and in vivo.

Wang XM, Xin MH, Xu J, Kang BR, Li Y, Lu SM, Zhang SQ.

Eur J Med Chem. 2015;96:382-95. doi: 10.1016/j.ejmech.2015.04.037. Epub 2015 Apr 17.

PMID:
25911625
20.

Discovery of potent and efficacious cyanoguanidine-containing nicotinamide phosphoribosyltransferase (Nampt) inhibitors.

Zheng X, Baumeister T, Buckmelter AJ, Caligiuri M, Clodfelter KH, Han B, Ho YC, Kley N, Lin J, Reynolds DJ, Sharma G, Smith CC, Wang Z, Dragovich PS, Oh A, Wang W, Zak M, Wang Y, Yuen PW, Bair KW.

Bioorg Med Chem Lett. 2014 Jan 1;24(1):337-43. doi: 10.1016/j.bmcl.2013.11.006. Epub 2013 Nov 14.

PMID:
24279990

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