3,4-Disubstituted isothiazoles: Novel potent inhibitors of VEGF receptors 1 and 2

3,4-Disubstituted isothiazoles: Novel potent inhibitors of VEGF receptors 1 and 2 Научная публикация

Журнал

Bioorganic & Medicinal Chemistry Letters
ISSN: 1464-3405 , E-ISSN: 0960-894X

Вых. Данные

Год: 2009, Том: 19, Номер: 4, Страницы: 1195-1198 Страниц : 4 DOI: 10.1016/j.bmcl.2008.12.078

Авторы

Kiselyov Alexander S. ¹ , Semenova Marina ² , Semenov Victor V. ³

Организации

1	deCODE, 2501 Davey Road, Woodridge, IL 60616, USA
2	Institute of Developmental Biology, RAS, 26 Vavilov Str., 119334 Moscow, Russia
3	Zelinsky Institute of Organic Chemistry, RAS, 47 Leninsky Prospect, 117913 Moscow, Russia

Novel derivatives of isothiazoles are described as potent ATP-competitive inhibitors of vascular endothelial growth factor receptors I and II (VEGFR-1/2). A number of compounds exhibited VEGFR-2 inhibitory activity comparable to that of Vatalanib™ in both HTRF enzymatic and cellular assays. Several derivatives featuring bulky meta-substituents in the amide portion of the molecule displayed 4- to 8-fold specificity for VEGFR-2 versus VEGFR-1. Active molecules also showed high intrinsic permeability (>30 × 10−5 cm/min) across Caco-2 cell monolayer.

Kiselyov A.S. , Semenova M. , Semenov V.V.
3,4-Disubstituted isothiazoles: Novel potent inhibitors of VEGF receptors 1 and 2
Bioorganic & Medicinal Chemistry Letters. 2009. V.19. N4. P.1195-1198. DOI: 10.1016/j.bmcl.2008.12.078 WOS Scopus OpenAlex

Web of science:	WOS:000263295200036
Scopus:	2-s2.0-59649112339
OpenAlex:	W2016872051

БД	Цитирований
OpenAlex	28
Scopus	28
Web of science	26