O
Osvaldo Dos Santos
Researcher at University of Connecticut
Publications - 22
Citations - 919
Osvaldo Dos Santos is an academic researcher from University of Connecticut. The author has contributed to research in topics: PI3K/AKT/mTOR pathway & Kinase. The author has an hindex of 14, co-authored 21 publications receiving 836 citations.
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Journal ArticleDOI
Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.
Aranapakam Mudumbai Venkatesan,Christoph Martin Dehnhardt,Efren Guillermo Delos Santos,Zecheng Chen,Osvaldo Dos Santos,Semiramis Ayral-Kaloustian,Gulnaz Khafizova,Natasja Brooijmans,Robert Mallon,Irwin Hollander,Larry Feldberg,Judy Lucas,Ker Yu,James Joseph Gibbons,Robert T. Abraham,Inder Chaudhary,Tarek S. Mansour +16 more
TL;DR: A series of bis(morpholino-1,3,5-triazine) derivatives were prepared and optimized to provide the highly efficacious PI3K/mTOR inhibitor 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)urea 26 (PKI-587).
Journal ArticleDOI
Antitumor Efficacy of PKI-587, a Highly Potent Dual PI3K/mTOR Kinase Inhibitor
Robert Mallon,Larry Feldberg,Judy Lucas,Inder Chaudhary,Christoph Martin Dehnhardt,Efren Guillermo Delos Santos,Zecheng Chen,Osvaldo Dos Santos,Semiramis Ayral-Kaloustian,Aranapakam Mudumbai Venkatesan,Irwin Hollander +10 more
TL;DR: Significant antitumor efficacy and a favorable pharmacokinetic/safety profile justified phase 1 clinical evaluation of PKI-587.
Journal ArticleDOI
Structure−Activity Relationship of 6-Methylidene Penems Bearing Tricyclic Heterocycles as Broad-Spectrum β-Lactamase Inhibitors: Crystallographic Structures Show Unexpected Binding of 1,4-Thiazepine Intermediates
Aranapakam M. Venkatesan,Yansong Gu,Osvaldo Dos Santos,T. Abe,Atul Agarwal,Youjun Yang,Petersen Peter J,William J. Weiss,Tarek S. Mansour,Michiyoshi Nukaga,Andrea M. Hujer,Robert A. Bonomo,James R. Knox +12 more
TL;DR: The design and synthesis of a series of seven tricyclic 6-methylidene penems as novel class A and C serine beta-lactamase inhibitors is described and the formation of the 1,4- thiazepine ring structures is proposed based on a 7-endo-trig cyclization.
Journal ArticleDOI
2,4-Diamino-quinazolines as inhibitors of β-catenin/Tcf-4 pathway: Potential treatment for colorectal cancer
Zecheng Chen,Aranapakam Mudumbai Venkatesan,Christoph Martin Dehnhardt,Osvaldo Dos Santos,Efren Guillermo Delos Santos,Semiramis Ayral-Kaloustian,Lei Chen,Yi Geng,K T Arndt,Judy Lucas,Inder Chaudhary,Tarek S. Mansour +11 more
TL;DR: Replacement of the biphenyl moiety in compound 1 with the N-phenylpiperidine-4-carboxamide chain resulted in a number of new analogues, which are potent inhibitors of the beta-catenin/Tcf-4 pathway.
Journal ArticleDOI
Lead Optimization of N-3-Substituted 7-Morpholinotriazolopyrimidines as Dual Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitors: Discovery of PKI-402
Christoph Martin Dehnhardt,Aranapakam Mudumbai Venkatesan,Efren Guillermo Delos Santos,Zecheng Chen,Osvaldo Dos Santos,Semiramis Ayral-Kaloustian,Natasja Brooijmans,Robert Mallon,Irwin Hollander,Larry Feldberg,Judy Lucas,Inder Chaudhary,Ker Yu,Jay Gibbons,Robert T. Abraham,Tarek S. Mansour +15 more
TL;DR: In vitro and in vivo biomarker studies demonstrated the ability of 3 to shut down the PI3K/Akt pathway and induce apoptosis in cancer cells, validating suppression of PI3k/mTOR signaling as a potential anticancer therapy.