- Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened
[作者:MUNCHHOF MICHAEL J; LI QIFANG; SHAVNYA ANDREI; BORZILLO GARY V; BOYDEN TRACEY L; JONES CHRISTOPHER S; LAGRECA SUSAN D; MARTINEZALSINA LUIS; PATEL NANDINI; PELLETIER KATHLEEN; REITER LARRY A; ROBBINS MICHAEL D; TKALCEVIC GEORGE T,期刊:ACS Medicinal Chemistry Letters, 页码:106-111 , 文章类型: Article,,卷期:2012年3-2]
- Inhibitors of the Hedgehog signaling pathway have generated a great deal of interest in the oncology area due to the mounting evidence of their potential to provide promising therapeutic options for patients. Herein, we ...
- Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria
[作者:HEIDEBRECHT RICHARD W JR; MULROONEY CAROL; AUSTIN CHRISTOPHER P; BARKER ROBERT H JR; BEAUDOIN JENNIFER A; CHENG KEN CHIHCHIEN; COMER EAMON; DANDAPANI SIVARAMAN; DICK JUSTIN; DUVALL JEREMY R; EKLAND ERIC H; FIDOCK DAVID A; FITZGERALD MARK E; FOLEY MICHAEL; GUHA RAJARSHI; HINKSON PAUL; KRAMER MARTIN; LUKENS AMANDA K; MASI DANIELA; MARCAURELLE LISA A; SU XINZHUAN; THOMAS CRAIG J; WEIWER MICHEL; WIEGAND ROGER C; WIRTH DYANN; XIA MENGHANG; YUAN JING; ZHAO JINGHUA; PALMER MICHELLE; MUNOZ BENITO; SCHREIBER STUART,期刊:ACS Medicinal Chemistry Letters, 页码:112-117 , 文章类型: Article,,卷期:2012年3-2]
- Here, we describe the discovery of a novel antimalarial agent using phenotypic screening of Plasmodium falciparum asexual blood-stage parasites. Screening a novel compound collection created using diversity-oriented synt...
- Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor
[作者:HADDACH MUSTAPHA; MICHAUX JEROME; SCHWAEBE MICHAEL K; PIERRE FABRICE; OBRIEN SEAN E; BORSAN COSMIN; TRAN JOE; RAFFAELE NICHOLAS; RAVULA SUCHITRA; DRYGIN DENIS; SIDDIQUIJAIN ADAM; DARJANIA LEVAN; STANSFIELD RYAN; PROFFITT CHRIS; MACALINO DIWATA; STREINER NICOLE; BLIESATH JOSHUA; OMORI MAY; WHITTEN JEFFREY P; ANDERES KENNA; RICE WILLIAM G; RYCKMAN DAVID M,期刊:ACS Medicinal Chemistry Letters, 页码:135-139 , 文章类型: Article,,卷期:2012年3-2]
- Structure activity relationship analysis in a series of 3-(5-((2-oxoindolin-3-ylidene)methyl)furan-2-yl)amides identified compound 13, a pan-Pim kinases inhibitor with excellent biochemical potency and kinase selectivity...
- Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models
[作者:ALBAUGH PAM; FAN YI; MI YUAN; SUN FANGXIAN; ADRIAN FRANCISCO; LI NANXIN; JIA YONG; SARKISOVA YELENA; KREUSCH ANDREAS; HOOD TAMI; LU MIN; LIU GUOXUN; HUANG SHENLIN; LIU ZUOSHENG; LOREN JON; TUNTLAND TOVE; KARANEWSKY DONALD S; SEIDEL H MARTIN; MOLTENI VALENTINA,期刊:ACS Medicinal Chemistry Letters, 页码:140-145 , 文章类型: Article,,卷期:2012年3-2]
- Neurotrophins and their receptors (TRKs) play key roles in the development of the nervous system and the maintenance of the neural network. Accumulating evidence points to their role in malignant transformations, chemota...
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