Novel N-phenylindazole based diarylureas have been designed, synthesized and evaluated as potential anticancer agents. In vitro cell viability studies of these derivatives illustrate good potency with IC50 values in the range of 0.4–50 μM in several cancer cell lines including murine metastatic breast cancer 4T1, murine glioblastoma GL261, human triple negative breast cancer MDA-MB-231, human pancreatic cancer MIAPaCa-2, and human colorectal cancer cell line WiDr. The ester group in the lead compound 8i was modified to incorporate amino-amides to increase solubility and stability while retaining biological activity. Further in vitro studies reveal that lead candidates inhibit tube length in HUVEC cells. In vivo systemic toxicity studies indicate that these candidate compounds are well tolerated in mice without any significant side effects. Anticancer efficacy studies in WiDr tumor xenograft and 4T1 tumor syngraft models demonstrate that the lead candidate 11 exhibits significant antitumor properties as a single agent in these tumor models.

Es wird über ein neues Verfahren zur Herstellung von organischen Rhodanverbindungen berichtet, das auf der direkten Umsetzung von Mercaptanen mit nascierendem Bromcyan in kaliumbromidgesättigtem Methanol beruht. Bei sehr oxydationsanfälligen Mercaptanen kann die Reaktion auch über das Disulfid erfolgen.

ChemInform Abstract Twenty-five thioxoquinazolinones such as (I) are S-alkylated with ethyl bromide (II) and subsequently coupled and rearranged with hydrazine hydrate (IV) to produce the title compounds (V).

No abstract

In dem ersten Teil der Übersicht werden Synthesen von aliphatischen Rhodan= Verbindungen, z.B. (III), durch Austausch von Halogen durch den Thiocyanatrest behandelt.