1-Piperazinylphthalazines as potential VEGFR-2 inhibitors and anticancer agents: Synthesis and in vitro biological evaluation was written by Abou-Seri, Sahar M.;Eldehna, Wagdy M.;Ali, Mamdouh M.;Abou El Ella, Dalal A.. And the article was included in European Journal of Medicinal Chemistry in 2016.Recommanded Product: 2103-99-3 This article mentions the following:
In our endeavor towards the development of effective VEGFR-2 inhibitors, three novel series of phthalazine derivatives based on 1-piperazinyl-4-arylphthalazine scaffold were synthesized. All the newly prepared phthalazines were evaluated in vitro for their inhibitory activity against VEGFR-2. In particular, compounds I and II potently inhibited VEGFR-2 at sub-micromolar IC50 values 0.35 ± 0.03 and 0.40 ± 0.04 μM, resp. Moreover, seventeen selected compounds were evaluated for their in vitro anticancer activity according to US-NCI protocol, where compounds I and II proved to be the most potent anticancer agents. While, compound I exhibited potent broad spectrum anticancer activity with full panel GI50 (MG-MID) value of 3.62 μM, compound II showed high selectivity toward leukemia and prostate cancer subpanels [subpanel GI50 (MG-MID) 3.51 and 5.15 μM, resp.]. Mol. docking of compounds I and II into VEGFR-2 active site was performed to explore their potential binding mode. In the experiment, the researchers used many compounds, for example, 4-(4-Chlorophenyl)thiazol-2-amine (cas: 2103-99-3Recommanded Product: 2103-99-3).
4-(4-Chlorophenyl)thiazol-2-amine (cas: 2103-99-3) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Recommanded Product: 2103-99-3
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica