- Structure-based design and synthesis of novel pseudosaccharine derivatives as antiproliferative agents and kinase inhibitors
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This study is concerned with the implementation of structure-based techniques for the design of new heterocyclic compounds based on pseudosaccharine scaffold with protein kinase inhibition activity. This nucleus was exploited based on the well-known quinazoline core and its interactions with several protein kinases. Two series of compounds employing this new scaffold were synthesized and evaluated at enzymatic and cellular levels. Compound 9b displayed broad spectrum antiproliferative activity on NCI 60-cell lines panel with mean GI50 of 5.4 μM. Investigation of the molecular mechanism showed probable inhibitory activity against Src kinase.
- Elsayed, Mohamed S.A.,El-Araby, Moustafa E.,Serya, Rabah A.T.,El-Khatib, Ahmed H.,Linscheid, Michael W.,Abouzid, Khaled A.M.
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p. 122 - 131
(2013/04/23)
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- HYDRAZONE DERIVATIVE
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A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 comb
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Page/Page column 58
(2009/10/06)
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- Design and synthesis of N-alkylated saccharins as selective α-1a adrenergic receptor antagonists
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Benign prostatic hyperplasia can be managed pharmacologically with α-1 adrenergic receptor antagonists. Agents that demonstrate selectivity for the α-la receptor subtype may offer advantages in clinical applications with respect to hypotensive side effect
- Nerenberg, Jennie B.,Erb, Jill M.,Thompson, Wayne J.,Lee, Hee-Yoon,Guare, James P.,Munson, Peter M.,Bergman, Jeffrey M.,Huff, Joel R.,Broten, Theodore P.,Chang, Raymond S. L.,Chen, Tsing B.,O'Malley, Stacey,Schorn, Terry W.,Scott, Ann L.
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p. 2467 - 2472
(2007/10/03)
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