Search Results - "Kalvin, Douglas"

Thrombospondin-1 Mimetic Peptide Inhibitors of Angiogenesis and Tumor Growth:  Design, Synthesis, and Optimization of Pharmacokinetics and Biological Activities by Haviv, Fortuna, Bradley, Michael F, Kalvin, Douglas M, Schneider, Andrew J, Davidson, Donald J, Majest, Sandra M, McKay, Laura M, Haskell, Catherine J, Bell, Randy L, Nguyen, Bach, Marsh, Kennan C, Surber, Bruce W, Uchic, John T, Ferrero, James, Wang, Yi-Chun, Leal, Juan, Record, Rae D, Hodde, Jason, Badylak, Stephen F, Lesniewski, Richard R, Henkin, Jack

“…The heptapeptide 1, NAc-Gly-Val-DIle-Thr-Arg-Ile-ArgNHEt, a structurally modified fragment derived from the second type-1 repeat of thrombospondin-1 (TSP-1),…”
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Structure−Activity Relationship Studies on N′-Aryl Carbohydrazide P2X7 Antagonists by Nelson, Derek W, Sarris, Kathy, Kalvin, Douglas M, Namovic, Marian T, Grayson, George, Donnelly-Roberts, Diana L, Harris, Richard, Honore, Prisca, Jarvis, Michael F, Faltynek, Connie R, Carroll, William A

“…N′-Aryl acyl hydrazides were identified as P2X7 receptor antagonists. Structure−activity relationship (SAR) studies evaluated functional activity by monitoring…”
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Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists by CARROLL, William A, KALVIN, Douglas M, PEREZ MEDRANO, Arturo, FLORJANCIC, Alan S, YING WANG, DONNELLY-ROBERTS, Diana L, NAMOVIC, Marian T, GRAYSON, George, HONORE, Prisca, JARVIS, Michael F

“…Structure-activity relationship (SAR) studies were conducted around early tetrazole-based leads 3 and 4. Replacements for the tetrazole core were investigated…”
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Discovery of a Series of Cyclohexylethylamine-Containing Protein Farnesyltransferase Inhibitors Exhibiting Potent Cellular Activity by Henry, Kenneth J, Wasicak, James, Tasker, Andrew S, Cohen, Jerome, Ewing, Patricia, Mitten, Michael, Larsen, John J, Kalvin, Douglas M, Swenson, Rolf, Ng, Shi-Chung, Saeed, Badr, Cherian, Sajeev, Sham, Hing, Rosenberg, Saul H

“…Synthesis of a library of secondary benzylic amines based on the Sebti−Hamilton type peptidomimetic farnesyltransferase (FTase) inhibitor FTI-276 (1) led to…”
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Scaffold oriented synthesis. Part 4: Design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions by Akritopoulou-Zanze, Irini, Wakefield, Brian D., Gasiecki, Alan, Kalvin, Douglas, Johnson, Eric F., Kovar, Peter, Djuric, Stevan W.

“…We report the synthesis and biological evaluation of 5-substituted indazoles as kinase inhibitors. The compounds were synthesized in a parallel synthesis…”
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Scaffold oriented synthesis. Part 3: Design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions by Akritopoulou-Zanze, Irini, Wakefield, Brian D., Gasiecki, Alan, Kalvin, Douglas, Johnson, Eric F., Kovar, Peter, Djuric, Stevan W.

“…We report the synthesis and biological evaluation of 5-substituted indazoles and amino indazoles as kinase inhibitors. The compounds were synthesized in a…”
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Microwave-Assisted Synthesis Utilizing Supported Reagents:  A Rapid and Efficient Acylation Procedure by Sauer, Daryl R, Kalvin, Douglas, Phelan, Kathleen M

“…The application of microwave heating to a polymer-assisted solution-phase (PASP) synthesis technique has been utilized to develop a rapid and efficient…”
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Synthesis of (4R)-D,L-[4-2H]- and (4S)-D,L-[42H]homoserine lactones by Kalvin, Douglas M, Woodard, Ronald W

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Synthesis of (1S,2R)- and (1S,2S)-1-amino[2-2H]cyclopropane-1-carboxylic acids: The total 1H NMR assignment of cyclo[ACC-.alpha.-methyl-Phe] by Subramanian, Pullachipatti K, Kalvin, Douglas M, Ramalingam, Kondareddiar, Woodard, Ronald W

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Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties by Kawai, Megumi, BaMaung, Nwe Y., Fidanze, Steve D., Erickson, Scott A., Tedrow, Jason S., Sanders, William J., Vasudevan, Anil, Park, Chang, Hutchins, Charles, Comess, Kenneth M., Kalvin, Douglas, Wang, Jieyi, Zhang, Qian, Lou, Pingping, Tucker-Garcia, Lora, Bouska, Jennifer, Bell, Randy L., Lesniewski, Richard, Henkin, Jack, Sheppard, George S.

“…Synthesis and biological activity of novel methionine aminopeptidase type -2 inhibitors having a sulfonamide bond are reported. We have screened molecules for…”
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Novel Antibacterial Class:  A Series of Tetracyclic Derivatives by Hinman, Mira M, Rosenberg, Teresa A, Balli, Darlene, Black-Schaefer, Candace, Chovan, Linda E, Kalvin, Douglas, Merta, Philip J, Nilius, Angela M, Pratt, Steve D, Soni, Niru B, Wagenaar, Frank L, Weitzberg, Moshe, Wagner, Rolf, Beutel, Bruce A

“…We describe the synthesis and antibacterial activity of a series of tetracyclic naphthyridones. The members of this series act primarily via inhibition of…”
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Structure−Activity Relationship Studies on N ′-Aryl Carbohydrazide P2X 7 Antagonists by Nelson, Derek W., Sarris, Kathy, Kalvin, Douglas M., Namovic, Marian T., Grayson, George, Donnelly-Roberts, Diana L., Harris, Richard, Honore, Prisca, Jarvis, Michael F., Faltynek, Connie R., Carroll, William A.

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Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X sub(7) antagonists by Carroll, William A, Kalvin, Douglas M, Medrano, Arturo Perez, Florjancic, Alan S, Wang, Ying, Donnelly-Roberts, Diana L, Namovic, Marian T, Grayson, George, Honore, Prisca, Jarvis, Michael F

“…Structure-activity relationship (SAR) studies were conducted around early tetrazole-based leads 3 and 4. Replacements for the tetrazole core were investigated…”
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Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4 H-1,2,4-triazole P2X 7 antagonists by Carroll, William A., Kalvin, Douglas M., Perez Medrano, Arturo, Florjancic, Alan S., Wang, Ying, Donnelly-Roberts, Diana L., Namovic, Marian T., Grayson, George, Honoré, Prisca, Jarvis, Michael F.

“…The synthesis and in vitro characterization of a series of phenyltriazole P2X 7 antagonists are described. Compound 12 was discovered to be active in a rat…”
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Novel inhibitors of bacterial protein synthesis: structure–activity relationships for 1,8-naphthyridine derivatives incorporating position 3 and 4 variants by Clark, Richard F., Wang, Sanyi, Ma, Zhenkun, Weitzberg, Moshe, Motter, Christopher, Tufano, Michael, Wagner, Rolf, Gu, Yu-Gui, Dandliker, Peter J., Lerner, Claude G., Chovan, Linda E., Cai, Yingna, Black-Schaefer, Candace L., Lynch, Linda, Kalvin, Douglas, Nilius, Angela M., Pratt, Steve D., Soni, Niru, Zhang, Tianyuan, Zhang, Xiaolin, Beutel, Bruce A.

“…Graphic Structure–activity relationships for a recently discovered novel ribosome inhibitor (NRI) class of antibacterials were investigated. Preliminary…”
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Potent and Selective Non-Cysteine-Containing Inhibitors of Protein Farnesyltransferase by Augeri, David J, O'Connor, Stephen J, Janowick, Dave, Szczepankiewicz, Bruce, Sullivan, Gerry, Larsen, John, Kalvin, Douglas, Cohen, Jerry, Devine, Edward, Zhang, Haichao, Cherian, Sajeev, Saeed, Badr, Ng, Shi-Chung, Rosenberg, Saul

“…Potent and selective non-thiol-containing inhibitors of protein farnesyltransferase are described. FTI-276 (1) was transformed into pyridyl ether analogue 19…”
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Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase by Augeri, David J., Janowick, Dave, Kalvin, Douglas, Sullivan, Gerry, Larsen, John, Dickman, Daniel, Ding, Hong, Cohen, Jerry, Lee, Jang, Warner, Robert, Kovar, Peter, Cherian, Sajeev, Saeed, Badr, Zhang, Haichao, Tahir, Steve, Ng, Shi-Chung, Sham, Hing, Rosenberg, Saul H.

“…Potent and orally bioavailable nonthiol-containing inhibitors of protein farnesyltransferase are described. Oral bioavailability was achieved by replacement of…”
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SYNTHESIS OF 4R- AND 4S- AND 3R- AND 3S-DEUTERATED HOMOSERINES. SYNTHESIS OF SPECIFICALLY-DEUTERATED 1-AMINOCYCLOPROPANE-1-CARBOXYLIC ACIDS by KALVIN, DOUGLAS MARK

“…This thesis describes the synthesis of 4R- and 4S-L- 4-('2)H(,1) homoserines, 3R- and 3S- 3-('2)H(,1) homoserines, and specifically-deuterated…”
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DNA breakage activity of the methanol extract of auromomycin by Kalvin, D M, Huang, C H, Lischwe, M A, Peters, E H, Prestayko, A W, Crooke, S T

“…The constituents of the antitumor agent auromomycin have been analyzed to determine their DNA-breakage activities. Spectral analysis showed that the methanol…”
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