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Discovery of Pyrido[3',2':5,6]thiopyrano[4,3-d]pyrimidine-Based Antiproliferative Multikinase Inhibitors.

ABSTRACT: Protein kinases dysregulation is extremely common in cancer cells, and the development of new agents able to simultaneously target multiple kinase pathways involved in angiogenesis and tumor growth may offer several advantages in the treatment of cancer. Herein we report the discovery of new pyridothiopyranopyrimidine derivatives (2-4) showing high potencies in VEGFR-2 KDR inhibition as well as antiproliferative effect on a panel of human tumor cell lines. Investigation on the selectivity profile of the representative 2-anilino-substituted compounds 3b, 3i, and 3j revealed a multiplicity of kinase targets that should account for the potent antiproliferative effect produced by these pyridothiopyranopyrimidine derivatives.

SUBMITTER: Salerno S 

PROVIDER: S-EPMC6466516 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature

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Discovery of Pyrido[3',2':5,6]thiopyrano[4,3-<i>d</i>]pyrimidine-Based Antiproliferative Multikinase Inhibitors.

Salerno Silvia S   Barresi Elisabetta E   García-Argáez Aída Nelly AN   Taliani Sabrina S   Simorini Francesca F   Amendola Giorgio G   Tomassi Stefano S   Cosconati Sandro S   Novellino Ettore E   Da Settimo Federico F   Marini Anna Maria AM   Dalla Via Lisa L  

ACS medicinal chemistry letters 20190117 4

Protein kinases dysregulation is extremely common in cancer cells, and the development of new agents able to simultaneously target multiple kinase pathways involved in angiogenesis and tumor growth may offer several advantages in the treatment of cancer. Herein we report the discovery of new pyridothiopyranopyrimidine derivatives (<b>2</b>-<b>4</b>) showing high potencies in VEGFR-2 KDR inhibition as well as antiproliferative effect on a panel of human tumor cell lines. Investigation on the sele  ...[more]

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