Leon M. Smith | Researchain

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Featured researches published by Leon M. Smith.

Bioorganic & Medicinal Chemistry | 2009

Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2

Matthew Duncton; Eugene L. Piatnitski Chekler; Reeti Katoch-Rouse; Dan Sherman; Wai C. Wong; Leon M. Smith; Joel Kawakami; Alexander S. Kiselyov; Daniel L. Milligan; Chris Balagtas; Yaron R. Hadari; Ying Wang; Sheetal Patel; Robin L. Rolster; James R. Tonra; David Surguladze; Stan Mitelman; Paul Kussie; Peter Bohlen; Jacqueline F. Doody

A series of arylphthalazine derivatives were synthesized and evaluated as antagonists of VEGF receptor II (VEGFR-2). IM-094482 57, which was prepared in two steps from commercially available starting materials, was found to be a potent inhibitor of VEGFR-2 in enzymatic, cellular and mitogenic assays (comparable activity to ZD-6474). Additionally, 57 inhibited the related receptor, VEGF receptor I (VEGFR-1), and showed excellent exposure when dosed orally to female CD-1 mice.

Synthetic Communications | 2006

Efficient Preparation of ((3‐Chloro‐2‐fluoro‐phenyl)‐[7‐methoxy‐8‐(3‐morpholin‐4‐yl‐propoxy)‐10,11‐dihydro‐5‐oxa‐2,4,11‐triaza‐dibenzo(a,d)cyclohepten‐1‐yl]‐amine) for In‐Vivo Study

Hu Liu; Leon M. Smith; Yunyu Mao; Weitao Pan; Yong-Jiang Xu; Sabina Burdzovic-Wizeman; Matthew Duncton; Wai C. Wong

Abstract An improved route for the preparation of highly functionalized 5,6‐dihydro‐pyrimido[4,5‐b][1,4]oxazepine 1a in multigram quantities was developed. This new methodology was highlighted by the proper methoxy disposition via a regioselective methylation of 2,4,5‐trihydroxy‐benzaldehyde followed by a magnesium sulfate–promoted cyclization.

Bioorganic & Medicinal Chemistry Letters | 2006

Oxadiazole derivatives as a novel class of antimitotic agents : Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines

Xiaohu Ouyang; Evgueni Piatnitski; Vatee Pattaropong; Xiaoling Chen; Hai-Ying He; Alexander S. Kiselyov; Avdhoot Velankar; Joel Kawakami; Marc Labelle; Leon M. Smith; Julia Winslow Lohman; Sui Ping Lee; Asra Malikzay; James Fleming; Jason Gerlak; Ying Wang; Robin L. Rosler; Kai Zhou; Stan Mitelman; Margarita Camara; David Surguladze; Jacqueline F. Doody; M. Carolina Tuma

Bioorganic & Medicinal Chemistry Letters | 2005

Synthesis and structure–activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors

Xiaohu Ouyang; Xiaoling Chen; Evgueni Piatnitski; Alexander S. Kiselyov; Hai-Ying He; Yunyu Mao; Vatee Pattaropong; Yang Yu; Ki Kim; John Kincaid; Leon M. Smith; Wai C. Wong; Sui Ping Lee; Daniel L. Milligan; Asra Malikzay; James Fleming; Jason Gerlak; Dhanvanthri S. Deevi; Jacqueline F. Doody; Hui-Hsien Chiang; Sheetal Patel; Ying Wang; Robin L. Rolser; Paul Kussie; Marc Labelle; M. Carolina Tuma

Bioorganic & Medicinal Chemistry Letters | 2006

Arylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II.

Matthew Duncton; Evgueni Piatnitski; Reeti Katoch-Rouse; Leon M. Smith; Alexander S. Kiselyov; Daniel L. Milligan; Chris Balagtas; Wai C. Wong; Joel Kawakami; Jacqueline F. Doody

Journal of Organic Chemistry | 2005

Preparation of substituted pyrimido[4,5-b]-1,4-benzoxazepines, thiazepines, and diazepines via a Pictet-Spengler cyclization.

Matthew Duncton; Leon M. Smith; Sabina Burdzovic-Wizeman; Aaron C. Burns; Hu Liu; Yunyu Mao; and Wai C. Wong; Alexander S. Kiselyov

Bioorganic & Medicinal Chemistry Letters | 2006

Novel tricyclic azepine derivatives: Biological evaluation of pyrimido[4,5-b]-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase

Leon M. Smith; Wai C. Wong; Alexander S. Kiselyov; Sabina Burdzovic-Wizemann; Yunyu Mao; Yong-Jiang Xu; Matthew Duncton; Ki Kim; Evgueni Piatnitski; Jacqueline F. Doody; Ying Wang; Robin L. Rosler; Daniel L. Milligan; John Columbus; Chris Balagtas; Sui Ping Lee; Andrey Konovalov; Yaron R. Hadari

Bioorganic & Medicinal Chemistry Letters | 2006

Tricyclic azepine derivatives: Pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors

Leon M. Smith; Evgueni Piatnitski; Alexander S. Kiselyov; Xiaohu Ouyang; Xiaoling Chen; Sabina Burdzovic-Wizemann; Yong-Jiang Xu; Ying Wang; Robin L. Rosler; Sheetal Patel; Hui-Hsien Chiang; Daniel L. Milligan; John Columbus; Wai C. Wong; Jacqueline F. Doody; Yaron R. Hadari

Archive | 2009

Substituted alkylamine derivative, and method for using the same

Jeffrey Adams; Jean E. Bemis; Shon Booker; Guolin Cai; Guoqing Chen; Michael Croghan; Lucian Dipietro; Celia Dominguez; Daniel Elbaum; Julie Germain; Stephanie Geuns-Meyer; Michael Handley; Qi Huang; Joseph L. Kim; Tae-Seong Kim; Alexander Kiselyov; Xiaohu Ouyang; Vinod F. Patel; Leon M. Smith; Markian Stec; Andrew Tasker; Ning Xi; Shimin Xu; Chester Chenguang Yuan; アレクサンダー・キセリヨフ; アンドリユー・タスカー; クオチン・チエン; クオリン・カイ; ジーン・ビーミス; ジエフリー・アダムズ

Archive | 2008

Substituted 2-amino-3-nicotin amide derivatives and pharmaceutical compositions comprising the same

Jeffrey Adams; Jean E. Bemis; Guoqing Chen; Lucian Dipietro; Celia Dominguez; Daniel Elbaum; Qi Huang; Joseph L. Kim; Xiaohu Ouyang; Vinod F. Patel; Leon M. Smith; Andrew Tasker; Ning Xi; Shimin Xu; Chester Chenguang Yuan; Michael Croghan; Julie Germain; Tae-Seong Kim

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