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Dive into the research topics where Diva Sze-Ming Chan is active.

Publication


Featured researches published by Diva Sze-Ming Chan.


Bioorganic & Medicinal Chemistry Letters | 2012

Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors.

Joerg Bussenius; Neel Kumar Anand; Charles M. Blazey; Owen Joseph Bowles; Lynne Canne Bannen; Diva Sze-Ming Chan; Baili Chen; Erick Wang Co; Simona Costanzo; Steven Charles Defina; Larisa Dubenko; Stefan Engst; Maurizio Franzini; Ping Huang; Vasu Jammalamadaka; Richard George Khoury; Moon Hwan Kim; Rhett Ronald Klein; Douglas Laird; Donna T. Le; Morrison B. Mac; David J. Matthews; David Markby; Nicole Miller; John M. Nuss; Jason Jevious Parks; Tsze H. Tsang; Amy Lew Tsuhako; Yong Wang; Wei Xu

The 70-kDa ribosomal protein S6 kinase (p70S6K) is part of the PI3K/AKT/mTOR pathway and has been implicated in cancer. High throughput screening versus p70S6K led to the identification of aminopyrimidine 3a as active inhibitor. Lead optimization of 3a resulted in highly potent, selective, and orally bioavailable pyrazolopyrimidines. In this manuscript we report the structure-activity relationship of this series and pharmacokinetic, pharmacodynamic, and efficacy data of the lead compound 13c.


Bioorganic & Medicinal Chemistry Letters | 2012

Pyrazolopyrimidines as dual Akt/p70S6K inhibitors.

Kenneth D. Rice; Moon Hwan Kim; Joerg Bussenius; Neel Kumar Anand; Charles M. Blazey; Owen Joseph Bowles; Lynne Canne-Bannen; Diva Sze-Ming Chan; Baili Chen; Erick Wang Co; Simona Costanzo; Steven Charles Defina; Larisa Dubenko; Stefan Engst; Maurizio Franzini; Ping Huang; Vasu Jammalamadaka; Richard George Khoury; Rhett Ronald Klein; A. Douglas Laird; Donna T. Le; Morrison B. Mac; David J. Matthews; David Markby; Nicole Miller; John M. Nuss; Jason Jevious Parks; Tsze H. Tsang; Amy Lew Tsuhako; Yong Wang

Activation of the PI3K/Akt/mTOR kinase pathway is frequently associated with human cancer. Selective inhibition of p70S6Kinase, which is the last kinase in the PI3K pathway, is not sufficient for strong tumor growth inhibition and can lead to activation of upstream proteins including Akt through relief of a negative feedback loop. Targeting multiple sites in the PI3K pathway might be beneficial for optimal activity. In this manuscript we report the design of dual Akt/p70S6K inhibitors and the evaluation of the lead compound 11b in vivo, which was eventually advanced into clinical development.


Bioorganic & Medicinal Chemistry Letters | 2014

Piperazinyl-oxadiazoles as selective sphingosine-1-phosphate receptor agonists.

Joshua Courtney Horan; Sulagna Sanyal; Younggi Choi; Melissa Hill-Drzewi; Lori Patnaude; Shawn Anderson; Steve Fogal; Can Mao; Brian Nicholas Cook; Kristina Gueneva-Boucheva; Michael B. Fisher; Eugene R. Hickey; Edward Pack; Lynne Canne Bannen; Diva Sze-Ming Chan; Morrison B. Mac; Stephanie Ng; Yong Wang; Wei Xu; Louise K. Modis; Rene Marc Lemieux

The discovery of a new series of selective S1P1 agonists is described. This series of piperazinyl-oxadiazole derivatives was rapidly optimized starting from high-throughput screening hit 1 to afford potent and selective lead compound 10d. Further SAR studies showed that 10d was converted to the active phosphate metabolite 29 in vivo. Oral administration of compound 10d to rats was shown to induce lymphopenia at 3 mg/kg.


Bioorganic & Medicinal Chemistry Letters | 2016

Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.

Joshua Courtney Horan; Daniel Kuzmich; Pingrong Liu; Darren Disalvo; John Lord; Can Mao; Tamara Denise Hopkins; Hui Yu; Christian Harcken; Raj Betageri; Melissa Hill-Drzewi; Lori Patenaude; Monica Patel; Kimberly Fletcher; Donna Terenzzio; Brian Linehan; Heather Xia; Mita Patel; Debbie Studwell; Craig Andrew Miller; Eugene R. Hickey; Jeremy I. Levin; Dustin Smith; Raymond A. Kemper; Louise K. Modis; Lynne Canne Bannen; Diva Sze-Ming Chan; Morrison B. Mac; Stephanie Ng; Yong Wang

Poor solubility and cationic amphiphilic drug-likeness were liabilities identified for a lead series of S1P3-sparing, S1P1 agonists originally developed from a high-throughput screening campaign. This work describes the subsequent optimization of these leads by balancing potency, selectivity, solubility and overall molecular charge. Focused SAR studies revealed favorable structural modifications that, when combined, produced compounds with overall balanced profiles. The low brain exposure observed in rat suggests that these compounds would be best suited for the potential treatment of peripheral autoimmune disorders.


Archive | 2004

c-Met modulators and methods of use

Lynne Canne Bannen; Diva Sze-Ming Chan; Jeff Chen; Lisa Esther Dalrymple; Timothy Patrick Forsyth; Tai Phat Huynh; Vasu Jammalamadaka; Richard George Khoury; James W. Leahy; Morrisson B. Mac; Grace Mann; Larry W. Mann; John M. Nuss; Jason Jevious Parks; Craig Stacy Takeuchi; Yong Wang; Wie Xu


Archive | 2005

Kinase modulators and methods of use

Neel Kumar Anand; Charles M. Blazey; Owen Joseph Bowles; Joerg Bussenius; Lynne Canne Bannen; Diva Sze-Ming Chan; Baili Chen; Erick Wang Co; Simona Costanzo; Steven Charles Defina; Larisa Dubenko; Maurizio Franzini; Ping Huang; Vasu Jammalamadaka; Richard George Khoury; Moon Hwan Kim; Rhett Ronald Klein; Donna T. Le; Morrison B. Mac; John M. Nuss; Jason Jevious Parks; Kenneth D. Rice; Tsze H. Tsang; Amy Lew Tsuhako; Yong Wang; Wei Xu


Archive | 2007

c-MET MODULATORS AND METHOD OF USE

Lynne Canne Bannen; Diva Sze-Ming Chan; Jeff Chen; Lisa Esther Dalrymple; Timothy Patrick Forsyth; Tai Phat Huynh; Vasu Jammalamadaka; Richard George Khoury; James W. Leahy; Morrison B. Mac; Grace Mann; Larry W. Mann; John M. Nuss; Jason Jevious Parks; Craig Stacy Takeuchi; Yong Wang; Wei Xu


Archive | 2005

Kinase modulators and method of use

Neel Kumar Anand; Charles M. Blazey; Owen Joseph Bowles; Joerg Bussenius; Bannen Lynne Canne; Diva Sze-Ming Chan; Baili Chen; Erick Wang Co; Simona Costanzo; Steven Charles Defina; Larisa Dubenko; Maurizio Franzini; Ping Huang; Vasu Jammalamadaka; Richard George Khoury; Moon Hwan Kim; Rhett Ronald Klein; Donna T. Le; Morrison B. Mac; John M. Nuss; Jason Jevious Parks; Kenneth D. Rice; Tsze H. Tsang; Amy Lew Tsuhako; Yong Wang; Wei Xu


Archive | 2009

Imidazo [1,2a] pyridine derivatives, their use as s1p1 agonists and methods for their production

Bannen Lynne Canne; Diva Sze-Ming Chan; Xiao-Hui Gu; Morrison B. Mac; Stephanie Ng; Tie-Lin Wang; Yong Wang; Wei Xu


Archive | 2005

Modulators of nuclear receptors

Christopher D. Bayne; Alan T. Johnson; Shao-Po Lu; Raju Mohan; Michael Charles Nyman; Edwin Schweiger; William C. Stevens; Haixia Wang; Yinong Xie; Lynne Canne Bannen; Diva Sze-Ming Chan; Ping Huang; Vasu Jammalamadaka; Richard George Khoury; Morrison B. Mac; Jason Jevious Parks; Yong Wang; Wei Xu

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